Novel Vanilloid Receptor Ligands and Use Thereof for the Production of Pharmaceutical Preparations

ABSTRACT

The present invention relates to novel vanilloid receptor ligands, to a process for the production thereof, to pharmaceutical preparations containing these compounds and to the use of these compounds for the production of pharmaceutical preparations.

CROSS-REFERENCE TO RELATED APPLICATIONS

The present application is a division of U.S. application Ser. No.11/551,060, filed, Oct. 19, 2006, which claims priority from 60/727,859,filed on Oct. 19, 2005, the disclosures of which are expresslyincorporated by reference therein

The present invention relates to novel vanilloid receptor ligands, to aprocess for the production thereof, to pharmaceutical preparationscontaining these compounds and to the use of these compounds for theproduction of pharmaceutical preparations.

The treatment of pain, in particular of neuropathic pain, is of greatsignificance in medicine. There is a worldwide need for effective paintreatments. The urgency of the requirement for effective therapeuticmethods for providing tailored and targeted treatment of chronic andnon-chronic pain, this being taken to mean pain treatment which iseffective and satisfactory from the patient's standpoint, is alsoevident from the large number of scientific papers relating to appliedanalgesia and to basic nociception research which have appeared inrecent times.

One suitable approach to the treatment of pain, in particular painselected from the group consisting of acute pain, chronic pain,neuropathic pain and visceral pain, particularly preferably ofneuropathic pain, is the vanilloid receptor subtype 1 (VR1/TRPV1), whichis also frequently known as the capsaicin receptor. This receptor isstimulated inter alfa by vanilloids such as for example capsaicin, heatand protons and plays a central role in the genesis of pain. It isfurthermore of significance to numerous other physiological andpathophysiological processes, such as for example migraine; depression;neurodegenerative diseases; cognitive disorders; anxiety states;epilepsy; coughing; diarrhea; pruritus; inflammation; disorders of thecardiovascular system; disorders of food intake; dependency onmedicines; abuse of medicines and in particular urinary incontinence.

One object of the present invention was accordingly to provide novelcompounds which are in particular suitable as pharmacological activeingredients in pharmaceutical preparations, preferably in pharmaceuticalpreparations for the treatment of disorders or diseases which are atleast in part mediated by vanilloid receptors 1 (VR1/TRPV1 receptors).

It has surprisingly now been found that the substituted compounds of thegeneral formula I stated below exhibit excellent affinity for thevanilloid receptor subtype 1 (VR1/TRPV1 receptor) and are thus inparticular suitable for the prevention and/or treatment of disorders ordiseases which at least in part mediated by vanilloid receptors 1(VR1/TRPV1). The substituted compounds of the general formulae A and Istated below also have an anti-inflammatory activity.

The present invention accordingly provides compounds of the generalformula A,

in whichX denotes O, S or N—C≡N;Y denotes —NH₂; —NHR³⁰; —NR³¹R³² or denote a linear or branched,saturated or unsaturated, unsubstituted or at least monosubstitutedaliphatic C₁₋₁₀ residue;n denotes 0, 1, 2, 3 or 4;R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl;Br; I; —SF₅; —NO₂; —CF₃; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote a linear orbranched, saturated or unsaturated, unsubstituted or at leastmonosubstituted aliphatic C₁₋₁₀ residue;R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³,—S(═O)₂—R²⁴; —S(═O)—R²⁴;denotes a linear or branched, unsaturated or saturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;or denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue, optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I;—SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³, —S(═O)—R²⁴; —S(═O)₂—R²⁴; or denote a linear orbranched, saturated or unsaturated, unsubstituted or at leastmonosubstituted aliphatic C₁₋₁₀ residue;or denote an unsubstituted or at least monosubstituted 6- or 10-memberedaryl residue, which may be attached via a linear or branched,substituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆alkenylene group or C₂₋₆ alkynylene group;R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂;—N═C(NHR²⁸)(NHR²⁹);denotes a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue and may be fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group;or denotes an unsubstituted or at least monosubstituted 5- to14-membered aryl or heteroaryl residue, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system and/or be attached via a linear orbranched, unsubstituted or at least monosubstituted C₁₋₆ alkylene groupor C₂₋₆ alkenylene group or C₂₋₆ alkynylene group;R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁸;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes a linear or branched, saturated orunsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀residue;R¹⁰ denotes —SF_(S); —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH;—C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH;—NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸;—S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴;—S(═O)²—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂;—N═C(NHR²⁸)(NHR²⁹);denotes a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀residue, which is in each case substituted with optionally 1, 2, 3, 4,5, 6, 7, 8 or 9 substituents mutually independently selected from thegroup consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃;denotes an unsubstituted C₂₋₁₀ alkenyle residue or an unsubstitutedC₂₋₁₀ alkynyle residue;denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue and may be fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group;or denotes an unsubstituted or at least monosubstituted 5- to14-membered aryl or heteroaryl residue, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system and/or be attached via a linear orbranched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group;R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³, R²⁴,R²⁷, R²⁸ and R²⁹, mutually independently, in each casedenote a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;denote an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue may be fused with a saturated or unsaturated,unsubstituted or at least monosubstituted mono- or polycyclic ringsystem and/or be attached via a linear or branched, unsubstituted or atleast monosubstituted C₁₋₆ alkylene group or 2- to 6-memberedheteroalkylene group;or denote an unsubstituted or at least monosubstituted 5- to 14-memberedaryl or heteroaryl residue, which may be fused with a saturated orunsaturated, unsubstituted or at least monosubstituted mono- orpolycyclic ring system and/or be attached via a linear or branched,unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to6-membered heteroalkylene group; orR¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a saturated or unsaturated,unsubstituted or at least monosubstituted 4-, 5-, 6-, 7-, 8- or9-membered heterocycloaliphatic residue, optionally comprising at leastone further heteroatom as ring member, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system; andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue;denote a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;or denote an unsubstituted or at least monosubstituted 5- to 14-memberedaryl or heteroaryl residue, which may be fused with a saturated orunsaturated, unsubstituted or at least monosubstituted mono- orpolycyclic ring system and/or be attached via a linear or branched,unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆alkenylene group or C₂₋₆ alkynylene group;or denote an unsaturated or saturated, unsubstituted or at leastmonosubstituted, 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶, together with the carbon atom joining them together as aring member, form a saturated or unsaturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5- or 6-membered cycloaliphatic residue;and R³⁰, R³¹ and R³², mutually independently, in each casedenote a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Unless otherwise stated, the above-stated aliphatic C₁₋₁₀ residues maypreferably optionally in each case be substituted with 1, 2, 3, 4, 5, 6,7, 8 or 9 substituents mutually independently selected from the groupconsisting of —C(═O)—O—C₁₋₅-alkyl, —O—C(═O)—C₁₋₅-alkyl, —O-phenyl,phenyl, F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅-alkyl),—S(C₁₋₅-alkyl), —N(C₁₋₅-alkyl)(C₁₋₅-alkyl), —OCF₃ and —SCF₃.

The above-stated C₁₋₆ alkylene groups, C₂₋₆ alkenylene groups and C₂₋₆alkynylene groups may preferably optionally in each case be substitutedwith 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independentlyselected from the group consisting of F, Cl, Br, I, —CN, —NO₂, —OH,—NH₂, —SH, —O(C₁₋₅-alkyl), —S(C₁₋₅-alkyl), —NH(C₁₋₅-alkyl),—N(C₁₋₅-alkyl)(C₁₋₅-alkyl), —OCF₃ and —SCF₃.

The term “heteroalkylene” denotes an alkylene group as stated above,wherein one or more carbon atoms are in each case replaced by aheteroatom mutually independently selected from the group consisting ofoxygen, sulfur and nitrogen (NH). Heteroalkylene groups may preferablycomprise 1, 2 or 3 heteroatom(s), more preferably one heteroatom,mutually independently selected from the group consisting of oxygen,sulfur and nitrogen (NH). Heteroalkylene groups may preferably be 2- to6-membered, more preferably 2- or 3-membered. —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—O—, —(CH₂)₂—O—, —(CH₂)₃—O—,—(CH₂)₄—O—(CH₂)—, —O—(CH₂)₂—, —O—(CH₂)₃—, —O—(CH₂)₄—, —C(C₂H₅)(H)—O—,—O—C(C₂H₅)(H)—, —CH₂—O—CH₂—, —CH₂—S—CH₂—, —CH₂—NH—CH₂—, —CH₂—NH— and—CH₂—CH₂—NH—CH₂—CH₂ may be mentioned by way of example of heteroalkylenegroups.

2- to 6-membered heteroalkylene groups may preferably optionally in eachcase be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituentsmutually independently selected from the group consisting of F, Cl, Br,I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅-alkyl), —NH(C₁₋₅-alkyl),—N(C₁₋₅-alkyl)(C₁₋₅-alkyl), —OCF₃ and —SCF₃.

The above-stated (hetero)cycloaliphatic residues may preferablyoptionally in each case be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of—C₁₋₆-alkylene-OH, ═CH₂, —O—C₁₋₅-alkylene-oxetanyl,—C₁₋₅-alkylene-O—C₁₋₅-alkylene-oxetanyl, —CH₂—N(C₁₋₅-alkyl)₂,—N[C(═O)—C₁₋₅-alkyl]-phenyl, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —O—C(═O)—C₁₋₅-alkyl, —NH₂, —NO₂, —S—CF₃,—SH, —C₁₋₅-alkyl, —C(═O)—C₁₋₅-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅-alkyl,—NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl,—N(C₁₋₅-alkyl)-phenyl, cyclohexyl, cyclopentyl, piperidinyl,pyrrolidinyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyland benzyl, wherein in each case the cyclic moiety of the residuesoxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,thiophenyl, phenethyl, —N[C(═O)—C₁₋₅-alkyl]-phenyl, —NH-phenyl,—N(C₁₋₅-alkyl)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl,—O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3,4 or 5 substituents mutually independently selected from the groupconsisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl,—O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl.

The above-stated (hetero)cycloaliphatic residues may likewise preferablyin each case optionally comprise 1, 2 or 3 (further) heteroatom(s)mutually independently selected from the group consisting of oxygen,nitrogen and sulfur.

The rings of the above-stated mono- or polycyclic ring systems maypreferably optionally in each case be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH,—O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —C₁₋₅-alkyl,—C(═O)—C₁₋₅-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl,—N(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein ineach case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyland benzyl may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl,—O—CF₃, —S—CF₃, phenyl and —O-benzyl.

The rings of the above-stated mono- or polycyclic ring systems arepreferably in each case 5-, 6- or 7-membered and may in each caseoptionally comprise 1, 2, 3, 4 or 5 heteroatom(s) as ring member(s),which are mutually independently selected from the group consisting ofoxygen, nitrogen and sulfur.

The above-stated aryl or heteroaryl residues may likewise preferablyoptionally in each case be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of F, Cl, Br,I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅-alkyl,—NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —NH—S(═O)₂—C₁₋₅-alkyl,—NH—C(═O)—O—C₁₋₅-alkyl, —C(═O)—H, —C(═O)—C₁₋₅-alkyl, —C(═O)—NH₂,—C(═O)—NH—C₁₋₅-alkyl, —C(═O)—N—(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN,—NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl.

The above-stated heteroaryl residues likewise preferably in each caseoptionally comprise 1, 2, 3, 4 or 5 heteroatom(s) mutually independentlyselected from the group consisting of oxygen, nitrogen and sulfur asring member(s).

If one or more of the above-stated residues denotes a saturated orunsaturated C₁₋₁₀ aliphatic residue, i.e. a C₁₋₁₀ alkyl, C₂₋₁₀ alkenylor C₂₋₁₀ alkynyl residue, the latter may preferably be substituted withoptionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutuallyindependently selected from the group consisting of —O-phenyl, F, Cl,Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —NH(C₁₋₅-alkyl),—N(C₁₋₅-alkyl)(C₁₋₅-alkyl), —C(═O)—O—C₁₋₅-alkyl, —OCF₃ and —SCF₃. C₂₋₁₀alkenyl residues comprise at least one, preferably 1, 2, 3 or 4 C—Cdouble bonds and C₂₋₁₀ alkynyl residues comprise at least one,preferably 1, 2, 3 or 4 C—C triple bonds.

alkyl residues are preferably selected from the group consisting ofmethyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, n-pentyl, 3-methyl-but-1-yl, 2-pentyl, 3-pentyl, sec-pentyl,neo-pentyl, 4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-yl, n-hexyl,n-heptyl, 2-heptyl, 3-heptyl, 4-heptyl, n-octyl, n-nonyl, 2-nonyl,3-nonyl, 4-nonyl, 5-nonyl and (2,6)-dimethyl-hept-4-yl, which mayoptionally be substituted in each case with 1, 2, 3, 4, 5, 6, 7, 8 or 9substituents mutually independently selected from the group consistingof —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂,—O—C(═O)—C(CH₃)₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, F,Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —OCF₃ and —SCF₃.

Alkenyl residues which are likewise preferred are those selected fromthe group consisting of vinyl, 1-propenyl, 2-propenyl, 1-butenyl,2-butenyl, 3-butenyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl,(3,3)-dimethyl-but-1-enyl, 2-methyl-buten-2-yl, 1-pentenyl, 2-pentenyl,3-pentenyl, 4-pentenyl, 1-hexenyl, 1-heptenyl and 1-octenyl, which mayoptionally be substituted in each case with 1, 2 or 3 substituentsmutually independently selected from the group consisting of F, Cl, Br,I, —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —OCF₃ and —SCF₃.

Alkynyl residues which are furthermore preferred are those selected fromthe group consisting of (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl,1-hexynyl, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl,3-butynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl and 4-pentynyl, which mayoptionally be substituted in each case with 1, 2 or 3 substituentsmutually independently selected from the group consisting of F, Cl, Br,I, —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃,—S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —OCF₃ and —SCF₃.

Particularly preferred optionally substituted C₁₋₁₀ aliphatic residuesare those selected from the group consisting of methyl, —CF₃, —CHF₂,—CH₂F, —CF₂Cl, —CCl₂F, —CCl₃, —CBr₃, —CH₂—CN, —CH₂—O—CH₃, —CH₂—O—CF₃,—CH₂—SF₃, —CH₂—NH₂, —CH₂—OH, —CH₂—SH, —CH₂—NH—CH₃, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—N(CH₃)(C₂H₅), ethyl, —CF₂—CH₃, —CHF—CF₂Cl,—CF₂—CFCl₂, —CFCl—CF₂Cl, —CFCl—CFCl₂, —CH₂—CH₂—NH₂, —CH₂—CH₂—OH,—CH₂—CH₂—SH, —CH₂—CH₂—NH—CH₃, —CH₂—CH₂—N(CH₃)₂, —CH₂—CH₂—N(C₂H₅)₂,—CH₂—CH₂—N(CH₃)(C₂H₅), —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃,—CH₂—CH₂—CN, n-propyl, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—SH,—CH₂—CH₂—CH₂—NH₂, —CH₂—CH₂—CH₂—NH—CH₃, —CH₂—CH₂—CH₂—N(CH₃)₂,—CH₂—CH₂—CH₂—N(C₂H₅)₂, —CH₂—CH₂—CH₂—N(CH₃)(C₂H₅), —CH₂—CH₂—O—CH₃,—CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, —CH₂—CH₂—CH₂—CN, —CH₂—O—CH₂—CH₃,—CH₂—CH₂—SF₃, —CH₂—CH₂—OCF₃, —CH(CH₃)(O—CH₃), —CH(CH₃)(S—CH₃), n-butyl,—CF₂—CF₂—CF₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CN, —CH₂—CH₂—CH₂—CF₃,—CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅,—CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—O—C₂H₅, —CH₂—C(═O)—O—C(CH₃)₃, —CH₂—CH₂—O—CH₃,—CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, sec-butyl,isobutyl, tert-butyl, n-pentyl, sec-pentyl, neo-pentyl, n-hexyl, vinyl,1-propenyl, 2-propenyl, 1-butenyl, 2-butenyl, 3-butenyl,2-methyl-buten-2-yl, (1,1,2)-trifluor-1-butenyl, 1-pentenyl, 2-pentenyl,3-pentenyl, 4-pentenyl, —CF═CF₂, —CCl═CCl₂, —CH₂—CF═CF₂, —CH₂—CCl═CCl₂,—C≡C—I, —C≡C—F and —C≡C—Cl.

If one or more of the above-stated substituents denotes a(hetero)cycloaliphatic residue, which may optionally be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system, the latter may preferably be selectedfrom the group consisting of cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, thiomorpholinyl,tetrahydropyranyl, oxetanyl, (1,2,3,6)-tetrahydropyridinyl, azepanyl,azocanyl, diazepanyl, dithiolanyl,(1,3,4,5)-tetrahydropyrido[4,3-b]indolyl,(3,4)-dihydro-1H-isochinolinyl, (1,3,4,9)-tetrahydro-M-carbolinyl and(1,3)-thiazolidinyl.

(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, (2,3)-dihydro-1H-indenyl,3-aza-bicyclo[3.1.1]heptyl, 3-aza-bicyclo[3.2.1]octyl,6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, isoindolyl,indolyl, (1,2,3,4)-tetrahydrochinolinyl,(1,2,3,4)-tetrahydroisochinolinyl, (2,3)-dihydro-1H-isoindolyl,(1,2,3,4)-tetrahydronaphthyl, (2,3)-dihydro-benzo[1.4]dioxinyl,benzo[1.3]dioxolyl, (1,4)-benzodioxanyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl,(3,4)-dihydro-2H-benzo[1.4]oxazinyl, octahydro-1H-isoindolyl andoctahydro-pyrrolo[3,4-c]pyrrolyl may be mentioned by way of example ofunsubstituted or at least mono-substituted (hetero)cycloaliphaticresidues which are fused with a saturated or unsaturated, unsubstitutedor at least monosubstituted mono- or polycyclic ring system.

According to the present invention (hetero)cycloaliphatic residues canform a spirocyclic residue together with a further(hetero)cycloaliphatic residue via a common carbon atom in both rings.

6-aza-spiro[2.5]octyl, 8-azaspiro[4.5]decyl and1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl may be mentioned by way of exampleof spirocyclic residue.

The (hetero)cycloaliphatic residues may particularly preferablyoptionally in each case be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of oxo (═O),thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —CH₂—OH, —CH₂—CH₂—OH,═CH₂, —CH₂—O—CH₂-oxetanyl, oxetanyl, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH-phenyl,—N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl,pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each casethe cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl,thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl,—N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl,—O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3,4 or 5 substituents mutually independently selected from the groupconsisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CF₃, phenyl and —O-benzyl.

If one or more of the above-stated substituents denotes an aryl residue,the latter may preferably be selected from the group consisting ofphenyl and naphthyl (1-naphthyl and 2-naphthyl).

If one or more of the above-stated substituents denotes a heteroarylresidue, the latter may preferably be selected from the group consistingof tetrazolyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl,pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl,benzo[b]furanyl, benzo[b]thiophenyl, benzoxazolyl, benzisoxazolyl,thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl,indazolyl, chinoxalinyl, chinolinyl and isochinolinyl.

isoindolyl, indolyl, (1,2,3,4)-tetrahydrochinolinyl,(1,2,3,4)-tetrahydroisochinolinyl, (2,3)-dihydro-1H-isoindolyl,(1,2,3,4)-tetrahydronaphthyl, (2,3)-dihydro-benzo[1.4]dioxinyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[1.3]dioxolyl and(1,4)-benzodioxanyl may be mentioned by way of example of unsubstitutedor at least monosubstituted aryl and heteroaryl residues which are fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system.

The aryl or heteroaryl residues may particularly preferably optionallyin each case be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂,—NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclicmoiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃,phenyl and —O-benzyl.

For the purposes of the present invention, a mono- or polycyclic ringsystem is taken to comprise mono- or polycyclic hydrocarbon residueswhich may be saturated or unsaturated and may optionally comprise 1, 2,3, 4 or 5 heteroatom(s) as ring member(s), which are mutuallyindependently selected from the group consisting of oxygen, nitrogen andsulfur. Such a mono- or polycyclic ring system may, for example, befused (anellated) with an aryl residue or a heteroaryl residue.

If a polycyclic ring system, such as for example a bicyclic ring system,is present, the various rings may in each case mutually independently beof a different degree of saturation, i.e. be saturated or unsaturated. Apolycyclic ring system is preferably a bicyclic ring system.

(1,3)-benzodioxolyl and (1,4)-benzodioxanyl may be mentioned by way ofexample of aryl residues which are fused with a mono- or polycyclic ringsystem.

If one or more of the above-stated substituents comprises a mono- orpolycyclic ring system, the latter may preferably be substituted with 1,2, 3, 4 or 5 substituents mutually independently selected from the groupconsisting of oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH,—O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃,—SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(O₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃,—C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein ineach case the cyclic moiety of the residues-O-phenyl, —O-benzyl, phenyland benzyl may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl,—O—CF₃, —S—CF₃, phenyl and —O-benzyl.

If one or more of the above-stated substituents comprises a linear orbranched C₁₋₆ alkylene group, the latter may preferably be selected fromthe group consisting of —(CH₂)—, —(CH₂)₂—, —C(H)(OH₃)—, —(CH₂)₃—,—(CH₂)₄—, —(OH₂)₅—, —C(H)(C(H)(CH₃)₂)— and —C(C₂H₅)(H)—.

Preferred substituted compounds are those of the above-stated generalformula A, in which

X denotes O;Y denotes —NH₂; —NHR³⁰; —NR³¹R³²; or denotes an alkyl residue selectedfrom the group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl,isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl;n denotes 1;R¹, R³ and R⁴ in each case denote H;R² denotes methyl; —O—CH₃; F; Cl; Br or I;R⁵ denotes a residue selected from the group consisting of methyl,ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F,—C(CH₃)₂(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F,—S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂ and —S—CH₂F;T denotes CH and U denotes CH and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes N and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes CH and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes N and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes CH and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes N and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes CH and V denotes CH and W denotes C—R¹⁰;R⁸ denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³;—OR¹⁴; —SR¹⁵;or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅,—CH₂—O—C(═O)—CH(CH₃)₂, n-butyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl,n-pentyl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl,(3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, pentynyl,butynyl, propynyl, ethynyl, 2-methyl-propen-1-yl,3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and(3,3)-dimethyl-but-1-enyl;or denotes a residues selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, indolyl,phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,thiophenyl, furanyl and pyridinyl, which may be in each case attached tothe parent structure via a —(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or in each case may optionally be substituted with 1, 2, 3, 4 or 5selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅,—OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃,—NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl and tert-butyl;R¹⁰ denotes —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;or a residue selected from the group consisting of phenyl, naphthyl,oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl andpyridinyl, which is in each case substituted with optionally 1, 2, 3, 4or 5 substituents selected from the group consisting of F, Cl, Br, I,—CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R¹¹, R¹², R¹³, R¹⁴ and R¹⁵, mutually independently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-bentenyl and 3-pentenyl;or denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, oxetanyl, piperidinyl, pyrrolidinyl,cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may be ineach case attached to the parent structure via a —CH₂—O—, —CH₂—CH₂—O—,—CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or in each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a radical selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, whereby theabove-stated residues in each case may optionally be substituted with 1,2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F,Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl; OrR¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which may optionally in eachcase be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of —CH₂—O—CH₂-oxetanyl,—O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃,—CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃,—CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂,—NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH,F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl,tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, piperidinyl,pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃,—(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case thecyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionallybe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl,Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl andsec-butyl; AndR²⁵ denotes an alkyl residue selected from the group consisting of—CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl,n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl or a residueselected from the group consisting of phenyl, benzyl, phenethyl,cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;R²⁶ denotes a hydrogen residue or a residue selected from the groupconsisting of methyl, ethyl and n-propyl; orR²⁵ and R²⁶, in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;And R³⁰, R³¹ and R³², mutually independently, in each case denote analkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃,methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl andisobutyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

The present invention also provides compounds of general formula I,

In whichX denotes O, S or N—C≡N;n denotes 0, 1, 2, 3 or 4;R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl;Br; I; —SF_(S); —NO₂; —CF₃; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂;—S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹;—NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹;—S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ ordenote a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³,—S(═O)₂—R²⁴; —S(═O)—R²⁴;

Denotes a linear or branched, unsaturated or saturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;

or denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue, optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸OrT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I;—SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³, —S(═O)—R²⁴; —S(═O)₂—R²⁴; or denote a linear orbranched, saturated or unsaturated, unsubstituted or at leastmonosubstituted aliphatic C₁₋₁₀ residue;or denote an unsubstituted or at least monosubstituted 6- or 10-memberedaryl residue, which may be attached via a linear or branched,substituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆alkenylene group or C₂₋₆ alkynylene group;R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂;—N═C(NHR²⁸)(NHR²⁹);

Denotes a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;

denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue and may be fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group;

Or denotes an unsubstituted or at least monosubstituted 5- to14-membered aryl or heteroaryl residue, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system and/or be attached via a linear orbranched, unsubstituted or at least monosubstituted C₁₋₆ alkylene groupor C₂₋₆ alkenylene group or C₂₋₆ alkynylene group;

R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁸;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes a linear or branched, saturated orunsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀residue;R¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂;—S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹;—NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹;—S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴;—C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹);denotes a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀residue, which is in each case substituted with optionally 1, 2, 3, 4,5, 6, 7, 8 or 9 substituents mutually independently selected from thegroup consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃;

Denotes an unsubstituted C₂₋₁₀ alkenyle residue or an unsubstitutedC₂₋₁₀ alkynyle residue;

denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue and may be fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group;

Or denotes an unsubstituted or at least monosubstituted 5- to14-membered aryl or heteroaryl residue, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system and/or be attached via a linear orbranched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group;

R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³, R²⁴,R²⁷, R²⁸ and R²⁹, mutually independently, in each case

Denote a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;

denote an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue may be fused with a saturated or unsaturated,unsubstituted or at least monosubstituted mono- or polycyclic ringsystem and/or be attached via a linear or branched, unsubstituted or atleast monosubstituted C₁₋₆ alkylene group or 2- to 6-memberedheteroalkylene group;

Or denote an unsubstituted or at least monosubstituted 5- to 14-memberedaryl or heteroaryl residue, which may be fused with a saturated orunsaturated, unsubstituted or at least monosubstituted mono- orpolycyclic ring system and/or be attached via a linear or branched,unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to6-membered heteroalkylene group; Or

R¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a saturated or unsaturated,unsubstituted or at least monosubstituted 4-, 5-, 6-, 7-, 8- or9-membered heterocycloaliphatic residue, optionally comprising at leastone further heteroatom as ring member, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system; AndR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue;

Denote a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;

Or denote an unsubstituted or at least monosubstituted 5- to 14-memberedaryl or heteroaryl residue, which may be fused with a saturated orunsaturated, unsubstituted or at least monosubstituted mono- orpolycyclic ring system and/or be attached via a linear or branched,unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆alkenylene group or C₂₋₆ alkynylene group;

Or denote an unsaturated or saturated, unsubstituted or at leastmonosubstituted, 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member;

Providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; Or

R²⁵ and R²⁶, together with the carbon atom joining them together as aring member, form a saturated or unsaturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5- or 6-membered cycloaliphatic residue;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Preferred compounds are those of above-stated general formulae A and I,in which

n, X, Y, T, U, V, W, R¹ to R⁷, R⁹ and R¹¹ to R³² have the meaning asdefined above;R⁸ denotes H; F; Cl; Br; I; —SF_(S); —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹;—S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴;—C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹);denotes a saturated or unsaturated, unsubstituted or at leastmonosubstituted chain comprising 1 to 7 carbon atoms as chain members,wherein 1, 2 or 3 carbon atoms can be replaced by heteroatoms selectedfrom the group consisting of oxygen, nitrogen (NH) and sulfur;denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue and may be fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group;or denotes an unsubstituted or at least monosubstituted 5- to14-membered aryl or heteroaryl residue, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system and/or be attached via a linear orbranched, unsubstituted or at least monosubstituted C₁₋₆ alkylene groupor C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; andR¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂;—S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH;—C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂;—C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹);denotes a saturated or unsaturated, unsubstituted or at leastmonosubstituted chain comprising 1 to 7 carbon atoms as chain members,wherein 1, 2 or 3 carbon atoms can be replaced by heteroatoms selectedfrom the group consisting of oxygen, nitrogen (NH) and sulfur, which, inthe absence of any heteroatoms as chain members, is substituted withoptionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutuallyindependently selected from the group consisting of —CN, —NO₂, —OH,—NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅ alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃;denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue and may be fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group;or denotes an unsubstituted or at least monosubstituted 5- to14-membered aryl or heteroaryl residue, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system and/or be attached via a linear orbranched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group.

Preferably the chain comprises 5 to 7 carbon atoms as chain members,wherein 1, 2 or 3 carbon atoms can be replaced by heteroatoms selectedfrom the group consisting of oxygen and sulfur.

If one or more of the above-stated residues denote a 1- to 7-memberedchain or a 5- to 7-membered chain, the latter may preferably besubstituted with optionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substitutentsmutually independently selected from the group consisting of—C₁₋₅-alkyl, F, Cl, Br, —CN, —NO₂, —OH, —NH₂, —SH, —S(C₁₋₅-alkyl),—NH(C₁₋₅-alkyl), —OCF₃, —SCF₃, —O-phenyl, —S-phenyl, —NH-phenyl,oxetanyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl,cyclopentyl and cyclohexyl, wherein in each case the cyclic moiety ofthe residues may be substituted with optionally 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —C(═O)—CH₂, —C(═O)—C₂H₅, phenyland —O-benzyl.

n-Pentyl, n-hexyl, 4-methyl-pent-1-ynyl, 1-hexynyl, pentynyl,1-pentenyl, 1-heptenyl, 1-hexenyl, —O—CH₂—CH₂—CH₂—O—CH₃,—S—CH₂—CH₂—CH₂—O—CH₃, —S—CH₂—CH₂—CH₂—S—CH₃,—O—CH₂—CH(CH₃)—O—CH₂-oxetanyl and —S—CH₂—CH(CH₃)—O—CH₂-oxetanyl may bementioned by way of example of 5- to 7-membered substituted orunsubstituted chains.

Preferred are those compounds of above-stated general formulae A and I,in which

X, n, R¹ to R²⁹, T, U, V and W have the meaning defined above;whereinunless otherwise stated, the above-stated aliphatic C₁₋₁₀ residues mayoptionally in each case be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9substituents mutually independently selected from the group consistingof F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅-alkyl),—S(C₁₋₅-alkyl), —NH(C₁₋₅-alkyl), —O—C(═O)—C₁₋₅-alkyl, —O-phenyl, phenyl,—OCF₃ and —SCF₃;the above-stated 2- to 6-membered heteroalkylene groups, C₁₋₆-alkylenegroups, C₂₋₆-alkenylene groups and C₂₋₆-alkynylene groups may optionallyin each case be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9substituents mutually independently selected from the group consistingof F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅-alkyl),—NH(C₁₋₅-alkyl), —N(C₁₋₅-alkyl)(C₁₋₅-alkyl), —OCF₃ and —SCF₃;the above-stated heteroalkylene groups may in each case optionallycomprise 1, 2 or 3 heteroatom(s) mutually independently selected fromthe group consisting of oxygen, nitrogen (NH) and sulfur;the above-stated (hetero)cycloaliphatic residues may optionally in eachcase be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of —C₁₋₆-alkylene-OH,═CH₂, —O—C₁₋₅-alkylene-oxetanyl,—C₁₋₅-alkylene-O—C₁₋₅-alkylene-oxetanyl, —CH₂—NH—C₁₋₅-alkyl,—CH₂—N(C₁₋₅-alkyl)₂, —N[C(═O)—C₁₋₅-alkyl]-phenyl, —CH₂—O—C₁₋₅-alkyl, oxo(═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl,—O—C(═O)—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—C₁₋₅-alkyl,—C₁₋₅-alkyl, —C(═O)—C₁₋₅-alkyl, —C(═O)—OH, —NH—C₁₋₅-alkyl, —NH-phenyl,—N(C₁₋₅-alkyl)-phenyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl,thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl,pyrrolidinyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyland benzyl, wherein in each case the cyclic moiety of the residuesoxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,thiophenyl, phenethyl, —N[C(═O)—C₁₋₅-alkyl]-phenyl, —NH-phenyl,—N(C₁₋₅-alkyl)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl,—O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3,4 or 5 substituents mutually independently selected from the groupconsisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl,—O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;and the above-stated (hetero)cycloaliphatic residues may in each caseoptionally comprise 1, 2 or 3 (further) heteroatom(s) mutuallyindependently selected from the group consisting of oxygen, nitrogen andsulfur;the rings of the above-stated mono- or polycyclic ring systems mayoptionally in each case be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of oxo (═O),thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂,—NO₂, —O—CF₃, —S—CF₃, —SH, —C₁₋₅-alkyl, —C(═O)—C₁₋₅-alkyl, —C(═O)—OH,—C(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —O-phenyl,—O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN,—NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl,and the rings of the above-stated mono- or polycyclic ring systems arein each case 5-, 6- or 7-membered and may in each case optionallycomprise 1, 2, 3, 4 or 5 heteroatom(s) as ring member(s), which aremutually independently selected from the group consisting of oxygen,nitrogen and sulfur;and the above-stated aryl or heteroaryl residues may optionally in eachcase be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —SH, —S—C₁₋₅-alkyl,—C₁₋₅-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅-alkyl, alkyl, —N(C₁₋₅-alkyl)₂,—NH—S(═O)₂—C₁₋₅-alkyl, —NH—C(═O)—O—C₁₋₅-alkyl, —C(═O)—H,—C(═O)—C₁₋₅-alkyl, —C(═O)—NH₂, —C(═O)—NH—C₁₋₅-alkyl,—C(═O)—N—(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, whereinin each case the cyclic moiety of the residues —O-phenyl, —O-benzyl,phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl,—O—CF₃, —S—CF₃, phenyl and —O-benzyl, andthe above-stated heteroaryl residues in each case optionally comprise 1,2, 3, 4 or 5 heteroatom(s) mutually independently selected from thegroup consisting of oxygen, nitrogen and sulfur as ring member(s);in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

The present invention also provides compounds of general formula B1,

in whichU, T, V, X, n, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have the meaning asdefined above;D denotes CH or N;p denotes 0, 1, 2 or 3;q denotes 0, 1, 2 or 3;K, L and M, mutually independently, in each case denote H, F, Cl, Br, I,—CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—C₁₋₅-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl,—NH—S(═O)₂—C₁₋₅-alkyl, —NH—C(═O)—O—C₁₋₅-alkyl, —C(═O)—H,—C(═O)—C₁₋₅-alkyl, —C(═O)—NH₂, —C(═O)—NH—C₁₋₅-alkyl,—C(═O)—N—(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, whereinin each case the cyclic moiety of the residues —O-phenyl, —O-benzyl,phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof F, Cl, Br, —OH, —CF₃, —SF_(S), —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl,—O—CF₃, —S—CF₃, phenyl and —O-benzyl;W denotes —CN, —NR³⁴R³⁵, —C(═O)—R³⁶ or —C(═O)—OR³⁷;and R³⁴, R³⁵, R³⁶ and R³⁷, mutually independently, in each case denotehydrogen or denote a linear or branched, saturated or unsaturatedaliphatic C₁₋₁₀ residuedenote an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue, which residue is in each case attached to the parent structurevia a carbon atom in the ring of the cycloaliphatic residue and may befused with a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group;or denote an unsubstituted or at least monosubstituted 5- to 14-memberedaryl or heteroaryl residue, which may be fused with a saturated orunsaturated, unsubstituted or at least monosubstituted mono- orpolycyclic ring system and/or be attached via a linear or branched,unsubstituted or at least monosubstituted C₁₋₆ alkylene group orC₂₋₆-alkenylene group or C₂₋₅-alkynylene group.

The present invention also provides compounds of general formula B2,

in whichU, T, V, X, n, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have the meaning asdefined above;D denotes CH or N;q denotes 0, 1, 2 or 3;K, L and M, mutually independently, in each case denote H, F, Cl, Br, I,—CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅-alkyl,—NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —NH—S(═O)₂—C₁₋₅-alkyl,—NH—C(═O)—O—C₁₋₅-alkyl, —C(═O)—H, —C(═O)—C₁₋₅-alkyl, —C(═O)—NH₂,—C(═O)—NH—C₁₋₅-alkyl, —C(═O)—N—(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF_(S),—CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and—O-benzyl;and R³⁴ and R³⁵, mutually independently, in each case denote hydrogen ordenote a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀residue;denote an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue, which residue is in each case attached to the parent structurevia a carbon atom in the ring of the cycloaliphatic residue and may befused with a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group;or denote an unsubstituted or at least monosubstituted 5- to 14-memberedaryl or heteroaryl residue, which may be fused with a saturated orunsaturated, unsubstituted or at least monosubstituted mono- orpolycyclic ring system and/or be attached via a linear or branched,unsubstituted or at least monosubstituted C₁₋₆ alkylene group orC₂₋₆-alkenylene group or C₂₋₆-alkynylene group.

Preferred compounds are those of above-stated general formulae I, B1 andB2, in which

X denotes O, S or N—C≡N;n denotes 0, 1, 2, 3 or 4;R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl;Br; I; —SF₅; —NO₂; —CN; —CF₃; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹;—C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote an alkylresidue selected from the group consisting of methyl, ethyl, n-propyl,isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyland n-heptyl;R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁶; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)—R²⁴; —S(═O)₂—R²⁴;denotes an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, n-hexyl and n-heptyl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl,cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichis in each case attached to the parent structure via a carbon atom ofthe rings of the above-stated residues and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo(═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl,—N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃,piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl,pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN,—NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃,phenyl and —O-benzyl;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I;—SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;—C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³, —S(═O)—R²⁴; —S(═O)₂—R²⁴; denote an alkylresidue selected from the group consisting of methyl, ethyl, n-propyl,isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyland n-heptyl or denote a phenyl residue, which may be attached via a—(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or may optionally besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅,—OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl andn-pentyl;R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)—R²⁴; —S(═O)₂—R²⁴, —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂;—N═C(NHR²⁸)(NHR²⁹);denotes an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl,(3,3)-dimethyl-but-1-yl, n-hexyl and n-heptyl;denotes an alkenyl residue selected from the group consisting of2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, (3,3)-dimethyl-but-1-enyl,ethenyl, propenyl, butenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and1-pentenyl;denotes an alkynyl residue selected from the group consisting ofethynyl, propynyl, butynyl, (3,3)-dimethyl-but-1-ynyl,4-methyl-pent-1-ynyl, 1-hexynyl and pentynyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl,cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichis in each case attached to the parent structure via a carbon atom ofthe rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or—C≡C—CH₂-group and may optionally in each case be substituted with 1, 2,3, 4 or 5 substituents mutually independently selected from the groupconsisting of —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃,—CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃,—CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅,—OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH,—C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl,—O—CH₂—CH₂—CH₂—CH₃, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃,—O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl,—O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues —NH-phenyl, —N(CH₃)— phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;or denotes a residue selected from the group consisting of tetrazolyl,phenyl, naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl,furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl,imidazolyl, indolyl, isoindolyl, benzo[b]furanyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]thiophenyl,benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl,pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyland isochinolinyl, wherein the residue may in each case be attached viaa —(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclicmoiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃,phenyl and —O-benzyl;R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —ON; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes an alkyl residue selected from thegroup consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl,n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl and n-heptyl;R¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂;—S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹;—NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹;—S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴;—C(═NH)—NH₂; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂;—N═C(NHR²⁸)(NHR²⁹);denotes an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, n-hexyl and n-heptyl which is in each case substituted withoptionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutuallyindependently selected from the group consisting of —CN, —NO₂, —OH,—NH₂, —SH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂,—N(C₂H₅)₂, —N(CH₃)(C₂H₅), —OCF₃ and —SCF₃;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl,cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichis in each case attached to the parent structure via a carbon atom ofthe rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or—C≡C—CH₂-group and may optionally in each case be substituted with 1, 2,3, 4 or 5 substituents mutually independently selected from the groupconsisting of —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃,—CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃,—CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅,—OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH,—C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl,—O—CH₂—CH₂—CH₂—CH₃, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃,—O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl,—O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues —NH-phenyl, —N(CH₃)— phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;or denotes a residue selected from the group consisting of tetrazolyl,phenyl, naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl,furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl,imidazolyl, indolyl, isoindolyl, benzo[b]furanyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]thiophenyl,benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl,pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyland isochinolinyl, wherein the residue may in each case be attached viaa —(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclicmoiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃,phenyl and —O-benzyl;R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³, R²⁴,R²⁷, R²⁸ and R²⁹, mutually independently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl,n-hexyl, n-heptyl, 3-pentyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl,cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, Cycloheptenyl,imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, wherein the residue may in each case be attachedvia a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂,—(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo(═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—O₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl,—N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃,piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl,pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN,—NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃,phenyl and —O-benzyl;or denote a residue selected from the group consisting of phenyl,naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl,pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl,imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl,benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl,pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyland isochinolinyl, wherein the residue may in each case be attached viaa —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH,—C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclicmoiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃,phenyl and —O-benzyl; orR¹² and R¹³ in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,3,4,5)-tetrahydropyrido[4,3-b]indolyl,(3,4)-dihydro-1H-isochinolinyl, (1,3,4,9)-tetrahydro-N-carbolinyl,imidazolidinyl, (1,3)-thiazolidinyl, piperazinyl, morpholinyl, azepanyl,diazepanyl and thiomorpholinyl, which may optionally in each case besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CH₂—O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —O—CH₂-oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo(═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, piperidinyl,pyrrolidinyl, cyclohexyl, cyclopentyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue;denote an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, n-hexyl and n-heptyl;denote a residue selected from the group consisting of phenyl, naphthyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl, pyrrolyl,pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl,indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl, benzoxazolyl,benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl,pyrimidinyl, indazolyl, chinoxalinyl, chinolinyl and isochinolinyl,wherein the residue may in each case be attached via a —(CH₂)—, —(CH₂)₂—or —(CH₂)₃-group and/or in each case may optionally be substituted with1, 2, 3, 4 or 5 substituents selected from the group consisting of F,Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl and n-pentyl;or denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶ in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,cyclopentenyl and cyclohexenyl;whereinunless otherwise stated, the above-stated alkyl, alkenyl and alkynylresidues may in each case optionally be substituted with 1, 2, 3, 4, 5,6, 7, 8 or 9 substituents mutually independently selected from the groupconsisting of alkenyl-C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂, —O—C(═O)—C(CH₃)₃,—O-phenyl, phenyl, F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂,—S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —OCF₃ and —SCF₃;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise preferred compounds are those of above-stated general formulaeA, I, B1 and B2, in which

X denotes O, S or N—C≡N;Y denotes —NH₂; —NHR³⁰; —NR³¹R³²; denotes an alkyl residue selected fromthe group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl,isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl;n denotes 0, 1, 2, 3 or 4;R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl;Br; I; —SF_(S); —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote a residue selected from thegroup consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl,—CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —O₂F₅, —CH₂—CCl₃, —CH₂—CBr₃,—CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R⁵ denotes F; Cl; Br; I; —SF_(S); —OR¹⁴; —SR¹⁵; —S(═O)—R²⁴; —S(═O)₂—R²⁴;denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CH₂—CN, —CH₂—O—CH₃,—CH₂—O—CF₃, —CH₂—SF₃, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃,—CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, —CH₂—CH₂—CN, n-propyl,—CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, —CH₂—CH₂—CH₂—CN, —CH₂—O—CH₂—CH₃,—CH₂—CH₂—SF₃, —CH₂—CH₂—OCF₃, —CH(CH₃)(O—CH₃), —CH(CH₃)(S—CH₃), n-butyl,—CF₂—CF₂—CF₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CN, n-butyl, sec-butyl, isobutyl,—C(CH₃)₂(CH₂OH), and tert-butyl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl,which may optionally in each case be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof oxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—O₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl andn-pentyl;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I;—SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH;—C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;—C(═O)—OR²²; —S(═O)—R²⁴; —S(═O)₂—R²⁴; denote a residue selected from thegroup consisting of —CH₂—OH, methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F,—CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃,—CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl or denote aphenyl residue, which may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof F, Cl, Br, I, —CN, —CF₃, SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl and n-pentyl;R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂;—S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹;—NR¹²R¹³; —OR¹⁴; —SR¹⁶; —C(═O)—OR²²; —S(═O)—R²⁴; —S(═O)₂—R²⁴;—C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹);or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, —CH₂—CH₂—CH₂—CF₃,—CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅,—CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅,—CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl,n-pentyl, sec-pentyl, neo-pentyl, n-hexyl, 2-methyl-propen-1-yl,3-methyl-but-2-en-1-yl, (3,3)-dimethyl-but-1-yl,(3,3)-dimethyl-but-1-enyl, ethenyl, propenyl, butenyl, 1-pentenyl,1-octenyl, 1-heptenyl, 1-hexenyl, (3,3)-dimethyl-but-1-ynyl,4-methyl-pent-1-ynyl, 1-hexynyl, ethynyl, propynyl, butynyl, pentynyl,—CF═CF₂, —CCl═Cl₂, —CH₂—CF═CF₂, —CH₂—CCl═CCl₂, —C≡C—I, —C≡C—F and—C≡C—Cl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, imidazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues or via a—(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, tetrazolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl,triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl,oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl,chinoxalinyl, chinolinyl and isochinolinyl, which may in each case beattached via a —(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or ineach case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl;R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂;—S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹;—NR¹²R¹³; —OR¹⁴; —SR¹⁵; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes a residueselected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CH₂F,—CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃,—CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R¹⁰ denotes —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—OR²²; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂;—C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹);denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, imidazolidinyl,tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues or via a—(CH═CH)—, or —C≡C—CH₂-group and may optionally in each case besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, tetrazolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl,triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl,oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl,chinoxalinyl, chinolinyl and isochinolinyl, which may in each case beattached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or in each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl;R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R²², R²⁴, R²⁷, R²⁸ and R²⁹, mutuallyindependently, in each casedenote a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CH₂—CN, —CH₂—O—CH₃,—CH₂—O—CF₃, —CH₂—SF₃, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃,—CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, —CH₂—CH₂—CN, n-propyl,—CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, —CH₂—CH₂—CH₂—CN, —CH₂—O—CH₂—CH₃,—CH₂—CH₂—SF₃, —CH₂—CH₂—OCF₃, —CH(CH₃)(O—CH₃), —CH(CH₃)(S—CH₃), n-butyl,—CF₂—CF₂—CF₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CN, sec-butyl, isobutyl, tert-butyl,n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl,cyclohexyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl,pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl,diazepanyl, azocanyl and thiomorpholinyl, which may in each case beattached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of oxo (═O), thioxo (═S), —OH,—O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl,triazolyl, pyridinyl, imidazolyl, thiazolyl, oxazolyl and isoxazolyl,which may in each case be attached via a —(CH₂)—, —(CH₂)₂— or—(CH₂)₃-group and/or in each case may optionally be substituted with 1,2, 3, 4 or 5 substituents selected from the group consisting of F, Cl,Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃,—NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂,—S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,isobutyl, tert-butyl, n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅,—NH—C(═O)—O—C(CH₃)₃, —C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂,—C(═O)—C(CH₃)₃, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅,—C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl andbenzyl; orR¹² and R¹³ in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl andthiomorpholinyl, which may optionally in each case be substituted with1, 2, 3, 4 or 5 substituents mutually independently selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂,—O—CH₂-oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—O₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo(═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —NH₂, —NO₂, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂,—S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, cyclohexyl,cyclopentyl, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of —CF₃, F, Cl, Br,—OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl, andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue;denote an alkyl residue selected from the group consisting of —CH₂—OH,—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl,sec-butyl, isobutyl, methyl, ethyl and n-propyl;denote a residue selected from the group consisting of phenyl, naphthyl,thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl,pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl, oxazolyl,isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl,chinoxalinyl, chinolinyl and isochinolinyl, which may in each case beattached via a —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶ in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;and R³⁰, R³¹ and R³², mutually independently, in each case denote analkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃,methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl andisobutyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Further preferred compounds are those of above-stated general formulaeA, I, B1 and B2, in which

X denotes O, S or N—C≡N;Y denotes —NH₂; —NHR³⁰; —NR³¹R³²; denotes an alkyl residue selected fromthe group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl,isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl;n denotes 0, 1 or 2;R¹, R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br;or denote a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂O₁, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl and —CFCl—CF₂Cl;R² denotes F; Cl; Br; I or denotes a residue selected from the groupconsisting of methyl, —CF₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,—CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl,—CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl,isobutyl, tert-butyl, —O—CH₃, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂,—O—CH₂F, —O—CF₂Cl, —O—C₂H₅, —O—CF₂—CH₃, —O—CH₂—CF₃, —O—C₂F₅,—O—CH₂—CCl₃, —O—CH₂—CBr₃, —O—CHF—CF₂Cl, —O—CF₂—CF₂Cl, —O—CFCl—CF₂Cl,—O—CH₂—CH₂—CH₃, —O—CF₂—CF₂—CF₃, —O—CF(CF₃)₂, —O—CH(CH₃)₂, —O—C(CH₃)₃,—S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F,—S—C₂H₅, —S—CF₂—CH₃, —S—CH₂—CF₃, —S—C₂F₅, —S—CH₂—CCl₃, —S—CH₂—CBr₃,—S—CHF—CF₂Cl, —S—CF₂—CF₂Cl, —S—CH₂—CH₂—CH₃, —S—CF₂—CF₂—CF₃, —S—CF(CF₃)₂,—S—CH(CH₃)₂ and —S—C(CH₃)₃;R⁵ denotes F; Cl; Br; I; —SF₅;or denotes a residue selected from the group consisting of methyl,ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CF₂—CH₃,—CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl,—CFCl—CF₂Cl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, sec-butyl, isobutyl,—C(CH₃)₂(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F,—O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —O—CH₂—CF₃, —O—C₂F₅, —O—CH₂—CCl₃,—O—CH₂—CBr₃, —O—CHF—CF₂Cl, —O—CF₂—CF₂Cl, —O—CFCl—CF₂Cl, —O—CF₂—CF₂—CF₃,—O—CF(CF₃)₂, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂,—S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S—CH₂—CF₃, —S—C₂F₅,—S—CH₂—CBr₃, —S—CHF—CF₂Cl, —S—CF₂—CF₂Cl, —S—CFCl—CF₂Cl, —S—CF₂—CF₂—CF₃,—S—CF(CF₃)₂, —S—CH(CH₃)₂, —S—C(CH₃)₃, —S(═O)₂—CF₃, —S(═O)₂—CCl₃,—S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F, —S(═O)₂—CF₂Cl, —S(═O)₂—CCl₂F,—S(═O)₂—CF₂—CH₃, —S(═O)₂—CH₂—CF₃, —S(═O)₂—C₂F₅, —S(═O)₂—CH₂—CCl₃,—S(═O)₂—CH₂—CBr₃, —S(═O)₂—CHF—CF₂Cl, —S(═O)₂—CF₂—CF₂Cl,—S(═O)₂—CFCl—CF₂Cl, —S(═O)₂—CF₂—CF₂—CF₃, —S(═O)₂—CF(CF₃)₂,—S(═O)₂—CH(CH₃)₂ and —S(═O)₂—C(CH₃)₃;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁶;R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I;—NO₂; —CN; —C(═O)—OCH₃; —C(═O)—OC₂H₅; or denote a residue selected fromthe group consisting of —CH₂—OH, methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂,—CH₂F, —CF₂Cl, —CCl₂F, ethyl, n-propyl, isopropyl, sec-butyl, isobutyland tert-butyl or denote a phenyl residue, which may optionally besubstituted in each case with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl andn-pentyl;R⁸ denotes H; F; Cl; Br; I; —OH; —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³;—OR¹⁴; —SR¹⁵; —C(═O)—OR²²;or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃,—CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl,3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, n-hexyl,(3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-ynyl,4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl,2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl,1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, phenyl, oxo (═O), thioxo (═S), methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl andn-pentyl;or denotes a residue selected from the group consisting of(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl;R⁹ denotes H; F; Cl; Br; I; —NO₂; —CN; or denotes a residue selectedfrom the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F,—CF₂Cl, —CCl₂F, ethyl n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl,sec-butyl, isobutyl and tert-butyl;R¹⁰ denotes —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;—C(═O)—OR²²;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S),methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl;R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²², mutually independently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl,cyclohexyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl,azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which may in eachcase be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl, pyrrolyl and pyridinyl, which may optionally be substituted ineach case with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅,—OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl; orR¹² and R¹³ in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl andthiomorpholinyl, which may optionally in each case be substituted with1, 2, 3, 4 or 5 substituents mutually independently selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo(═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, cyclohexyl,cyclopentyl, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of —CF₃, F, Cl, Br,—OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue; denote an alkyl residue selected from the group consisting of—CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl,n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl or denote aresidue selected from the group consisting of phenyl, benzyl, phenethyl,cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶ in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;and R³⁰, R³¹ and R³², mutually independently, in each case denote analkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃,methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl andisobutyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise preferred compounds are those of above-stated general formulaeI, B1 and B2, in which

X denotes O or S;n denotes 0, 1 or 2;R¹, R³ and R⁴ in each case denote H;R² denote F; Cl; Br; I or denote a residue selected from the groupconsisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃,—O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃,—S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F;R⁵ denotes F; Cl; Br; I; —SF₅;denotes a residue selected from the group consisting of methyl, ethyl,—CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂(CH₂OH),tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl,—O—CCl₂F, —O—CF₂—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F,—S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃,—S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷ in each case denote —CF₃; phenyl; —C(═O)—OCH₃; —C(═O)—OC₂H₅;methyl; —CH₂—OH; H; F; Cl; Br and I;R⁸ denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³;—OR¹⁴; —SR¹⁵; —C(═O)—OR²²;denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃,—CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl,n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, 4-methyl-pent-1-yl,(3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl,ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl,3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and(3,3)-dimethyl-but-1-enyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S),methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl and n-pentyl;or denote a residue selected from the group consisting of(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —C≡O—, —(CH₂)—, —(CH₂)₂— or —(OH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl;R⁹ denotes —CF₃; H; F; Cl; Br or I;R¹⁰ denotes —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;—C(═O)—OR²²;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S),methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl;R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²², mutually independently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, n-pentyl, 3-pentyl,n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl,3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃,—CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl,propenyl, 2-butenyl, 3-butenyl, 2-pentenyl, 3-pentenyl and tert-butyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,oxetanyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in each casebe attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF3, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR¹² and R¹³ in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl andthiomorpholinyl, which may optionally in each case be substituted with 1or 2 substituents mutually independently selected from the groupconsisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo(═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, cyclohexyl,cyclopentyl, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of —CF₃, F, Cl, Br,—OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue; denote an alkyl residue selected from the group consisting of—CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl,n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl or denote aresidue selected from the group consisting of phenyl, benzyl, phenethyl,cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶ in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclo pentyl, cyclohexyl andcycloheptyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise preferred compounds are those of above-stated general formulaeI, B1 and B2, in which

X denotes O;n denotes 1;R¹, R³ and R⁴ in each case denote H;R² denote methyl; —O—CH₃; F; Cl; Br or I;R⁵ denote a residue selected from the group consisting of methyl, ethyl,—CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂(CH₂OH),tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CF₃, —S—CCl₃,—S—CBr₃, —S—CHF₂ and —S—CH₂F;or denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;T denotes CH and U denotes CH and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes N and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes CH and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes N and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes CH and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes N and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes CH and V denotes CH and W denotes C—R¹⁰;R⁸ denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³;—OR¹⁴; —SR¹⁵;or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃,—CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl,3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, n-pentyl, n-hexyl,(3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-ynyl,4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl,2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl,1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S),methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl and n-pentyl;or denotes a radical selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl;R¹⁰ denotes —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—O₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S),methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl and n-pentyl;or denotes a radical selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl substituted;R¹¹, R¹², R¹³, R¹⁴ and R¹⁵, mutually independently, in each casedenotes a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denotes a radical selected from the group consisting of2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,oxetanyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in each casebe attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a radical selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which may in eachcase optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR¹² and R¹³ in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which may optionally in eachcase be substituted with 1 or 2 substituents mutually independentlyselected from the group consisting of —CH₂—O—CH₂-oxetanyl,—O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃,—CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃,—CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂,—NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH,F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl,tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, piperidinyl,pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃,—(CH₂)-pyridinyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, pyridinyl, phenyl andbenzyl, wherein in each case the cyclic moiety of the residues oxetanyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl,—N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl,—O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl,n-propyl, n-butyl, tert-butyl and sec-butyl; andR²⁵ denotes an alkyl residue selected from the group consisting of—CH₂—OH, —CH₂—CH₂—OH, methyl, ethyl and n-propyl or denotes a residueselected from the group consisting of benzyl, phenyl, phenethyl,cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;R²⁶ denote a hydrogen residue or denote a residue selected from thegroup consisting of methyl, ethyl and n-propyl; orR²⁵ and R²⁶ in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Ia1,

in whichX^(a) denotes O or S;na denotes 0, 1 or 2;R^(2a) denotes F; Cl; Br; I or denotes a residue selected from the groupconsisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃,—O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃,—S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F;R^(5a) denotes F; Cl; Br; I; —SF_(S);denotes a residue selected from the group consisting of methyl, ethyl,—CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂—(CH₂OH),tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl,—O—CCl₂F, —O—CF₂—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F,—S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃,—S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;R^(8a) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11a);—NR^(12a)R^(13a); —OR^(14a); —SR^(15a); —C(═O)—OR^(22a);or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃,CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, 3-methyl-but-1-yl,4-methyl-pent-1-yl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl,(3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl,ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl,3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and(3,3)-dimethyl-but-1-enyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S),methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH,—O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃,—NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11a), R^(12a), R^(13a), R^(14a), R^(15a) and R^(22a), mutuallyindependently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl, which may in each case beattached via a —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and—C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of —CF₃, F, Cl, Br,—O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,isobutyl and tert-butyl; orR^(12a) and R^(13a) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which may optionally in eachcase be substituted with 1 or 2 substituents mutually independentlyselected from the group consisting of —CH₂—O—CH₂-oxetanyl,—O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃,—CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃,—CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂,—NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH,F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl,tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl,thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl,pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃,—(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case thecyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl,thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl,—N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl,—O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl,n-propyl, n-butyl, tert-butyl and sec-butyl;R^(25a) and R^(26a), mutually independently, in each case denote ahydrogen residue; denote a residue selected from the group consisting of—CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl,n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl;providing that R^(25a) and R^(26a) do not in each case denote a hydrogenresidue; orR^(25a) and R^(26a) in each case together with the carbon atom joiningthem together as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Ia,

in whichX^(a), na, R^(5a), R^(8a) and R^(2a) have the meaning as defined above;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise particularly preferred compounds are those of general formulaIa, in which

X^(a) denotes O or S;na denotes 0, 1 or 2;R^(2a) denotes F; Cl; Br; I or denotes a residue selected from the groupconsisting of methyl, —CF₃, —CCl₃, —CBr₃, —CH₂F, —O—CH₃, —O—CF₃,—O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃,—S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F;R^(5a) denotes F; Cl; Br; I; —SF₅;denotes a residue selected from the group consisting of methyl, ethyl,—CF₃, —CCl₃, —CBr₃, —C(CH₃)₂—(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃,—O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —S—CF₃,—S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃,—S(═O)₂—CCl₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;R^(8a) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11a);—NR^(12a)R^(13a); —OR^(14a); —SR^(15a); —C(═O)—OR^(22a);or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃,—CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl,3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, n-hexyl,(3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-ynyl,4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl,2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl,1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S),methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, indolyl,phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,thiophenyl, furanyl and pyridinyl, which may in each case be attachedvia a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or ineach case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂,—NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11a), R^(12a), R^(13a), R^(14a), R^(15a) and R^(22a), mutuallyindependently, in each casedenote a radical from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl,n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl,3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃,—CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl,propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a radical selected from the group consisting of2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, oxetanyl, cyclopentyl and cyclohexyl, which may in each casebe attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12a) and R^(13a) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of

In case the synthesis of the above-stated residues in position of thesubstituents R¹² and R¹³ is not given in the experimental part, suchsynthesis are known to those skilled in the art.

Particularly preferred compounds are those of general formula Cl,

in whichna, R^(2a), R^(25a), R^(26a), R^(5a) and X^(a) have the meaning asdefined above;D denotes CH or N;pa denotes 0,qa denotes 0, 1 or 2;Ka, La and Ma, mutually independently, in each case denote H, —CF₃, —OH,—O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl,tert-butyl or sec-butyl;Wa denotes —NR^(34a)R^(35a), —CN, —C(═O)—R^(36a) or —C(═O)—OR^(37a);and R^(34a), R^(35a), R^(36a) and R^(37a), mutually independently, ineach case denote H or denote a residue selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl andisobutyl.

Likewise particularly preferred compounds are those of general formulaC2,

in whichna, R^(2a), R^(5a) and X^(a) have the meaning as defined above;D denotes CH or N;qa denotes 0, 1 or 2;Ka, La and Ma, mutually independently, in each case denote H, —CF₃, —OH,—O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl,tert-butyl or sec-butyl;and R^(34a) and R^(35a), mutually independently, in each case denote Hor denote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl and isobutyl.

Particularly preferred compounds are those of general formula Ib1,

in whichnb denotes 0, 1 or 2;R^(2b) denotes methyl; —O—CH₃; F; Cl; Br or I;R^(8b) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11b);NR^(12b)R^(13b); —OR^(14b); —SR^(15b);denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃,—CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, n-pentyl, n-hexyl,(3,3)-dimethyl-but-1-yl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl,(3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl,ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl,3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and(3,3)-dimethyl-but-1-enyl;denotes a residue from the group consisting of cyclopropyl, cyclobutyl,cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues or via a—(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S),methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —C≡O—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl;R^(11b), R^(12b), R^(13b), R^(14b) and R^(15b), mutually independently,in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH_(s), —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl,—CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyland 3-pentenyl;denote a residue selected from the group consisting of oxetanyl,2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl, which may in each case beattached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which mayoptionally be substituted in each case with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12b) and R^(13b) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which may optionally in eachcase be substituted with 1 or 2 substituents mutually independentlyselected from the group consisting of —CH₂—O—CH₂-oxetanyl,—O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN,—CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃,—CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂,—NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH,F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂,—O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl,tert-butyl, sec-butyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, cyclohexyl, cyclopentyl,piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅,—O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl,wherein in each case the cyclic moiety of the residues oxetanyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, —N[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl,—N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl,—O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl,n-propyl, n-butyl, tert-butyl and sec-butyl;R^(25b) and R^(26b), mutually independently, in each case denote ahydrogen residue; denote an alkyl residue selected from the groupconsisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH,—CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl,ethyl and n-propyl;providing that R^(25b) and R^(26b) do not in each case denote a hydrogenresidue; orR^(25b) and R^(26b) in each case together with the carbon atom joiningthem together as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Ib,

in whichnb, R^(8b) and R^(2b) have the meaning as defined above;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Ib, inwhich

nb denotes 1;R^(2b) denotes F;R^(8b) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11b);—NR^(12b)R^(13b); —OR^(14b); —SR^(15b);denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃,—CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl,n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, 3-methyl-but-1-yl,4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl,1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl,3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and(3,3)-dimethyl-but-1-enyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or may optionally ineach case be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂,—NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11b), R^(12b), R^(13b), R^(14b) and R^(15b), mutually independently,in each casedenote a residue selected from the group consisting of —(CH₂)-pyridinyl,—(CH₂)₂-pyridinyl, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl,n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl,n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅,—CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl,3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, oxetanyl, piperidinyl, pyrrolidinyl,cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in eachcase be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12b) and R^(13b) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which in each case mayoptionally be substituted with 1 or 2 substituents selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃,—NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃,—O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl,isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl,—O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃,—(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case thecyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl,(1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl andbenzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of —CF₃, —OH,—O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl,tert-butyl and sec-butyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Ic1,

in whichnc denotes 0, 1 or 2;R^(2c) denotes methyl; —O—CH₃; F; Cl; Br or I;R^(8c) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11c);—NR^(12c)R^(13c); —OR^(14c); —SR^(15c);denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅,—CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl,—CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl,—CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, CH₂—O—C(═O)—C₂H₅,—CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, n-pentyl, n-hexyl,(3,3)-dimethyl-but-1-yl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl,(3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl,ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl,3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and(3,3)-dimethyl-but-1-enyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which may in each case be attached via a—(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl;R^(11c), R^(12c), R^(13c), R^(14c) and R^(15c), mutually independently,in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, oxetanyl, cyclopentyl and cyclohexyl, which may in each casebe attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12c) and R^(13c) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-aza-spiro[2.5]octyl,3-aza-aza-bicyclo[3.2.1]octyl, 6-aza-aza-bicyclo[3.3.1]heptyl,8-aza-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which in each case mayoptionally be substituted with 1 or 2 substituents selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃,—NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃,—O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl,isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl,cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl,pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionallybe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl,Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl andsec-butyl;R^(25c) and R^(26c), mutually independently, in each case denote ahydrogen residue; or denote a residue selected from the group consistingof —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH,isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl;providing that R^(25c) and R^(26c) do not in each case denote a hydrogenresidue; orR^(25c) and R^(26c) in each case together with the carbon atom joiningthem together as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Ic,

in whichnc, R^(8c) and R^(2c) have the meaning as defined above;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise particularly preferred compounds are those of general formulaIc, in which

nc denotes 1;R^(2c) denotes F;R^(8c) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11c);—NR^(12c)R^(13c); —OR^(14c); —SR^(15c);denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃,—CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃,—CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl,n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, 3-methyl-but-1-yl,4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl,1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl,3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and(3,3)-dimethyl-but-1-enyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, wherein the residue may in each case be attachedvia a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or ineach case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂,—NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11c), R^(12c), R^(13c), R^(14c), and R^(15c), mutually independently,in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, oxetanyl, cyclopentyl and cyclohexyl, wherein the residuemay in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—,—CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or in each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12c) and R^(13c) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which in each case mayoptionally be substituted with 1 or 2 substituents selected from thegroup consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅,—N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo(═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃,—O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl,n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃,—O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl andbenzyl, wherein in each case the cyclic moiety of the residues oxetanyl,—N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl,thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl,—N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl,—O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl,n-propyl, n-butyl, tert-butyl and sec-butyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Id1,

in whichX^(d) denotes O or S;nd denotes 0, 1 or 2;R^(2d) denotes F; Cl; Br; I or denotes a residue selected from the groupconsisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃,—O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃,—S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F;R^(5d) denotes F; Cl; Br; I; —SF₅;denotes a residue selected from the group consisting of methyl, ethyl,—CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂—(CH₂OH),tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl,—O—CCl₂F, —O—CF₂—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F,—S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃,—S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;R^(10d) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11d); —NR^(12d)R^(13d);—OR^(14d); —SR^(15d); —C(═O)—OR^(22d);denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—O₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, indolyl,phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,thiophenyl, furanyl and pyridinyl, wherein the residue may in each casebe attached via a —(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/orin each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂,—NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11d), R^(12d), R^(13d), R^(14d), R^(15d), and R^(22d), mutuallyindependently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, oxetanyl, cyclopentyl and cyclohexyl, wherein the residuemay in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—,—CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or in each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, phenyl, naphthyl, thiophenyl,furanyl, pyrrolyl and pyridinyl, which in each case may optionally besubstituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; orR^(12d) and R^(13d) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which in each case mayoptionally be substituted with 1 or 2 substituents selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃,—NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃,—O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl,isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl,cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl,pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionallybe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl,Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl andsec-butyl;R^(25d) and R^(26d), mutually independently, in each case denote ahydrogen residue; or denote an alkyl residue selected from the groupconsisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH,—CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl,ethyl and n-propyl;providing that R^(25d) and R^(26d) do not in each case denote a hydrogenresidue; orR^(25d) and R^(26d) in each case together with the carbon atom joiningthem together as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Id,

in whichX^(d), nd, R^(2d), R^(5d) and R^(10d) have the meaning as defined above;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Ie1,

in whichne denotes 0, 1 or;R^(2e) denotes methyl; —O—CH₃; F; Cl; Br or I;R^(10e) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11e); —NR^(12e)R^(13e);—OR^(14e); —SR^(15e);denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, wherein the residue may in each case be attachedvia a —(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH,—O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃,—NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11e), R^(12e), R^(13e), R^(14e) and R^(15e), mutually independently,in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of oxetanyl,2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl, wherein the residue may in eachcase be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12e) and R^(13e) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which in each case mayoptionally be substituted with 1 or 2 substituents selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃,—NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃,—O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl,isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl,cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl,pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionallybe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl,Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl andsec-butyl;R^(25e) and R^(26e), mutually independently, in each denote a hydrogenresidue; or denote an alkyl residue selected from the group consistingof —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH,isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl;providing that R^(25e) and R^(26e) do not in each case denote a hydrogenresidue; orR^(25e) and R^(26e) in each case together with the carbon atom joiningthem together as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula Ie,

in whichne, R^(10e) and R^(2e) have the meaning as defined above,in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise particularly preferred compounds are those of general formulaIe, in which

ne denotes 1;R^(2e) denotes F;

R^(10e) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11e); —NR^(12e)R^(13e);—OR^(14e); —SR^(15e);

denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of tetrazolyl,(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, wherein the residue may in each case be attachedvia a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or ineach case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂,—NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11e), R^(12e), R^(13e), R^(14e) and R^(15e), mutually independently,in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of oxetanyl,2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl, wherein the residue may in eachcase be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—O₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12e) and R^(13e) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which in each case mayoptionally be substituted with 1 or 2 substituents selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃,—NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃,—O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl,isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl,cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl,pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues oxetanyl, N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionallybe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl,Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl andsec-butyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula If1,

in whichnf denotes 0, 1 or 2;R^(2f) denotes methyl; —O—CH₃; F; Cl; Br or I;R^(10f) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11f); —NR^(12f)R^(13f);—OR^(14f); —SR^(15f);denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, wherein the residue may in each case be attachedvia a —(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅,—NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl and tert-butyl;R^(11f), R^(12f), R^(13f), R^(14f) and R^(15f), mutually independently,in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of oxetanyl,2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl, wherein the residue may in eachcase be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12f) and R^(13f) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which in each case mayoptionally be substituted with 1 or 2 substituents selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃,—NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃,—O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl,isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl,cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl,thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl,—O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl,pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues oxetanyl, —N[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionallybe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl,Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl andsec-butyl;R^(25f) and R^(26f), mutually independently, in each case denote ahydrogen residue; or denote an alkyl residue selected from the groupconsisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH,—CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl,ethyl and n-propyl;providing that R^(25f) and R^(26f) do not in each case denote a hydrogenresidue; orR^(25f) and R^(26f) in each case together with the carbon atom joiningthem together as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl andcycloheptyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of general formula If,

in whichnf, R^(10f) and R^(2f) have the meaning as defined above;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise particularly preferred compounds are those of general formulaIf, in which

nf denotes 1;R^(2f) denotes F;R^(10f) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11f); —NR^(12f)R^(13f);—OR^(14f); —SR^(15f);denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyland thiomorpholinyl, which is in each case attached to the parentstructure via a carbon atom of the rings of the above-stated residues orvia a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂,—CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl;or denotes a residue selected from the group consisting of(1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl,(2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, wherein the residue may in each case be attachedvia a —(CH═CH)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH,—O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃,—NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11f), R^(12f), R^(13f), R^(14f) and R^(15f), mutually independently,in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;denote a residue selected from the group consisting of oxetanyl,2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl, wherein the residue may in eachcase be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—,—CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, tert-butyl, n-pentyl, n-hexyl,—C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of—(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in eachcase may optionally be substituted with 1, 2, 3, 4 or 5 substituentsselected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl andtert-butyl; orR^(12f) and R^(13f) in each case together with the nitrogen atom joiningthem together as a ring member, form a residue selected from the groupconsisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl,3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl,8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl,azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl,(4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl,piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which in each case mayoptionally be substituted with 1 or 2 substituents selected from thegroup consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH,—CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl,—N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —CH₂—O—CH₃, —NH₂,—NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl,—N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃,—O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl,isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, piperidinyl,pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃,—(CH₂)-pyridinyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl,thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, pyridinyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl,(4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl,phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl,—(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionallybe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl,Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl andsec-butyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Very particularly preferred compounds are those of general formula Ig,

in whichng denotes 0, 1 or 2;R^(2g) denotes methyl; —O—CH₃; F; Cl; Br or I;R^(14g) denotes a residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;T denotes CH and U denotes N and V denotes CH orT denotes N and U denotes CH and V denotes CH orT denotes N and U denotes N and V denotes CH orT denotes N and U denotes CH and V denotes N orT denotes CH and U denotes N and V denotes N;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise very particularly preferred compounds are those of generalformula Ig, in which

ng denotes 1;R^(2g) denotes F;R^(14g) denotes a residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl,(2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl,—CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃,ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl;T denotes CH and U denotes N and V denotes CH orT denotes N and U denotes CH and V denotes CH orT denotes N and U denotes N and V denotes CH orT denotes N and U denotes CH and V denotes N orT denotes CH and U denotes N and V denotes N;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Still further preferred compounds of the above-stated general formulaeare those selected from the group consisting of

-   [1]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-methyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [2]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [3]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [4]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-fluoro-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [5]    N-((2-chloro-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [6]    N-((-bromo2-bromo-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [7]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-iodo-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [8]    N-((2-tert-butyl-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [9]    N-((2-cyano-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [10]    (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [11]    (R)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [12]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-morpholino-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [13]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [14]    N-((2-(dimethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [15]    N-((2-(diethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [16]    N-((2-(dipropylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [17]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-hydroxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [18]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-methoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [19]    N-((2-butoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [20]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-isopropoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [21]    N-((2-cyclopentyloxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [22]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-phenyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [23]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(4-fluoro-phenyl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [24]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((6-(trifluoromethyl)-2,2′-bipyridin-3-yl)methyl)propanamide-   [25]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((6-(trifluoromethyl)-2,3′-bipyridin-3-yl)methyl)propanamide-   [26]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pyrimidin-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [27]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(thiazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [28]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(oxazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [29]    N-((2-(1H-imidazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [30]    N-(2-cyano-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [31]    (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [32]    (R)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [33]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-morpholino-4-(trifluoromethyl)benzyl)propanamide-   [34]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [35]    N-(2-(dimethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [36]    N-(2-(diethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [37]    N-(2-(dipropylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [38]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-hydroxy-4-(trifluoromethyl)benzyl)propanamide-   [39]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-methoxy-4-(trifluoromethyl)benzyl)propanamide-   [40]    N-(2-butoxy-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [41]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-isopropoxy-4-(trifluoromethyl)benzyl)propanamide-   [42]    N-(2-(cyclopentyloxy)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [43]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide-   [44]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N4(4′-fluoro-5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide-   [45]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-2-yl)-4-(trifluoromethyl)benzyl)propanamide-   [46]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-3-yl)-4-(trifluoromethyl)benzyl)propanamide-   [47]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrimidin-2-yl)-4-(trifluoromethyl)benzyl)propanamide-   [48]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(thiazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide-   [49]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(oxazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide-   [50]    N-(2-(1H-imidazol-2-yl)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [51]    N-((6-tert-butyl-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [52]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N4(4-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [53]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((3-(piperidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide-   [54]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N4(4-(piperidin-1-yl)-2-(trifluoromethyl)pyrimidin-5-yl)methyl)propanamide-   [55]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N4(3-(piperidin-1-yl)-5-(trifluoromethyl)pyrazin-2-yl)methyl)propanamide-   [56]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((4-(piperidin-1-yl)-6-(trifluoromethyl)pyridazin-3-yl)methyl)propanamide-   [57]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)propanamide-   [58]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperidin-1-yl)-4-(trifluoromethyl)phenyl)propanamide-   [59]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)ethyl)propanamide-   [60]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenethyl)propanamide-   [61]    N-(2-amino-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [62]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-nitro-4-(trifluoromethyl)benzyl)propanamide-   [63]    N-(4-tert-butyl-2-(piperidin-1-yl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [64]    2-(3-chloro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [65]    2-(3-chloro-4-(methylsulfonamido)phenyl)-N-((2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [66]    2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [67]    2-(3-bromo-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [68]    2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [69]    2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [70]    N-(4-tert-butyl-2-cyanobenzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [71]    N-((6-(chlorodifluoromethyl)-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-(4-methylsulfonamido)phenyl)propanamide-   [72]    (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-morpholino-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [73]    N-((2-(4-benzylpiperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [74]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide;-   [75]    N-(2-chloro-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [76]    N-((2-(cyclohexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl-2-(3-fluoro-4-methylsulfonamido)phenyl)propanamide-   [77]    N-((3-chloro-5-(trifluoromethyl)pyridin-2-yl)methyl-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [78]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((3-(pyrrolidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide-   [79]    N-((2-(3,5-dimethylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [80]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [81]    N-((2-(azepan-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [82]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(4-methylpiperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide;-   83    (S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-propionamide-   84    (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-propionamide-   85    N-(2-dimethylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   87    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-imidazol-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   88    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-thiophen-2-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   89    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   90    N-(2-cyclohexylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   91    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   93    (S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   94    (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   95    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   96    (S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   97    (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   98    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-4-trifluoromethyl-benzyl)-propionamide-   99    (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-4-trifluoromethyl-benzyl)-propionamide-   100    N-(2-cyclopropylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   101    N-(2-cyclobutylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   102    2-(3-chloro-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   103    2-(3-bromo-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   104    N-(4-benzyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   106    N-(2-benzyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   107    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methoxy-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   108    N-(2-butoxy-4-tert-butyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   109    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   110    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   111    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-propoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   112    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   113    N-[2-(4-chloro-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   114    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-fluoro-4-trifluoromethyl-benzyl)-propionamide-   115    N-(2-benzylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   116    N-(2-butylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   117    N-[2-(4-tert-butyl-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   118    N-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   120    (S)—N-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   121    (R)—N-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   122    N-(2-butylsulfanyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   123    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   124    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-methyl-cyclopropylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   125    N-[2-(3,3-dimethyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   126    N-(2-cyclohexylsulfanyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   127    2-(4-methylsulfonamido-3-methyl-phenyl)-N-(6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   128    N-(2-azocan-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   129    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-4-trifluoromethyl-benzyl)-thiopropionamide-   130    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-thiopropionamide-   131    N-[6′-(chloro-difluoro-methyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   132    N-[2-azepan-1-yl-6-(chlor-difluor-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   133    N-(4-tert-butyl-2-isobutoxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   134    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   135    N-[2-(3,4-dimethyl-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   136    N-[2-(5-chloro-2-methyl-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   137    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   138    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-fluoro-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   139    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   140    N-[2-butoxy-6-(chlor-difluor-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   142    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   144    (S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   145    (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   147    N-[2-(4-chloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   148    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   149    N-[2-(3-chloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   150    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   151    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   152    N-[4-tert-butyl-2-(2,2-dimethyl-propoxy)-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   153    N-(4-tert-butyl-2-pentyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   154    N-(4-tert-butyl-2-cyclohexyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   155    N-(4-tert-butyl-2-cyclopentyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   156    N-(2-cyclobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   157    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   158 acetic    acid-3′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-yl    ester-   159    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   160    N-(4-butoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   161    N-(2-cyclopentylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   162    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-isopropoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   163    N-(2-ethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   164    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6″-trifluoromethyl-3,4,5,6,3′,4′,5′,6′-octahydro-2H,2′H-[1,4′;1′,2″]terpyridin-3″-ylmethyl)-propionamide-   165    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-pyrrolidin-1-yl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   166    N-[6-(chloro-difluoro-methyl)-2-cyclopentyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   167    N-[2-(butyl-methyl-amino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   168    N-[6-(chloro-difluoro-methyl)-2-cyclohexyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   169    N-[2-benzyloxy-6-(chlor-difluor-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   170    N-[2-(4-tert-butyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   171    N-[2-(4-ethyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   172    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   173    N-[2-(4-chloro-benzylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   174    N-(2-azepan-1-yl-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   175    N-[2-(4-fluoro-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   176    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-pyridin-4-yl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   177    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-4-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   178    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenethyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   179    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide-   180    N-[6-(chloro-difluoro-methyl)-2-hexyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   181    N-[6-(chloro-difluoro-methyl)-2-(pyridin-3-ylmethoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   182    N-[6-(chloro-difluoro-methyl)-2-(pyridin-2-ylmethoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   183    N-(2-dibutylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   184    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6′-(4-fluoro-phenyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide-   185    N-[2-azepan-1-yl-6-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   186    N-[6-(chloro-difluoro-methyl)-2-dipropylamino-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   187    N-[6′-(chloro-difluoro-methyl)-3,5-dimethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   188    N-[2-(1,3-dihydro-isoindol-2-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   189    3′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-carbonic    acid ethylester-   190    N-(4,6′-bis-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   191    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-styryl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   192    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenethyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   193    N-{2-[4-(3-chloro-pyridin-2-yl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   194    N-{2-[4-(3-chloro-pyridin-2-yl)-2-methyl-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   195    N-(4,6′-bis-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide-   196    2-(4-methylsulfonamido-3-methyl-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   197    N-(4-ethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   198    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   199    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methoxymethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   200    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide-   201    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide-   202    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-2-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   203    2-(4-methylsulfonamido-3-methyl-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   204    N-(2-benzyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide-   205    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(methyl-phenyl-amino)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   206    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-trifluoromethyl-2-(4-trifluoromethyl-benzyloxy)-benzyl]-propionamide-   207    N-[6-(chloro-difluoro-methyl)-2-(4-phenyl-piperazin-1-yl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   208    N-[6-(chloro-difluoro-methyl)-2-isobutoxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   209    N-(2-benzyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   210    N-(4,4-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   211    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-3-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   212    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(3-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-pyridin-3-ylmethyl}-propionamide-   213    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(3-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-pyridin-3-ylmethyl}-propionamide-   214    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-pyridin-2-yl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   215    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   216    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide-   217    N-(2-azocan-1-yl-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   218    N-[2-(4,4-dimethyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   219    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-p-tolyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   220    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-m-tolyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   221    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide-   222    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-pyridin-3-ylmethyl}-propionamide-   223    N-(2-benzyloxy-4-hydroxymethyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   225    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   226 2,2-dimethyl-propionic    acid-3′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-yl    ester-   227    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-oxo-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   228    N-(4-ethoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   229    N-[2-(4-ethyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   230    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-trifluoromethyl-2-(4-trifluoromethyl-piperidin-1-yl)-benzyl]-propionamide-   231    N-[2-(4-benzyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   233    N-(6-tert-butyl-2-cyclohexyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   234    N-(6-tert-butyl-2-cyclopentyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   235    N-(2-butoxy-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   236    N-(6-tert-butyl-2-hexyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   237    N-(2-benzyloxy-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   238    N-(2-cyclohexyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   239    (R)—N-(2-cyclohexyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   240    N-(6-tert-butyl-2-pyrrolidin-1-yl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   241    N-(6′-tert-butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   242    N-[2-(4-ethyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   243    N-[2-(4-butyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   244    N-[2-(4-tert-butyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   245    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(indan-2-yloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   246    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-p-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide-   247    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-m-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide-   248    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{4-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-benzyl}-propionamide-   249    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-4-trifluoromethyl-benzyl}-propionamide-   250    N-[2-(3,4-dichloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   251    N-[2-(3-tert-butyl-1-oxa-2,8-diaza-spiro[4.5]dec-2-en-8-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   252    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-phenyl-1-oxa-2,8-diaza-spiro[4.5]dec-2-en-8-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   253    2-(3-fluoro-4-(pentafluorsulfanylsulfonamido)phenyl)-N-p-tolylpropanamid-   254    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-fluoro-4-methoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   255    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-fluoro-phenyl)-piperidin-1-yl]-4-trifluoromethyl-benzyl}-propionamide-   256    N-(2-butoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide-   257    N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide-   258    N-[2-(4-chloro-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   259    N-(4-dimethylaminomethyl-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   260    N-[2-(4-cyclohexyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   261    N-(6-tert-butyl-2-cyclopentyloxy-4-hydroxymethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   262    2-(4-methylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   263    N-[2-(3,3-dimethyl-butyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   264    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-p-tolyl-ethyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   265    N-[2-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   266    N-(2-benzo[1,3]dioxol-5-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   267    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   268    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-pentyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   269    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-hydroxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   270    N-(2-cyclohexylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   271    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-cyclohexylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   272    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methylsulfonamido-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   273    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-methyl-propenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   274    N-[2-(3,3-dimethyl-but-1-enyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   275    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1H-indol-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   276    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1H-indol-5-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   277    N-[2-(4-chloro-3-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   278    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-3-methyl-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   279    N-[2-(2,2-dimethyl-cyclopropylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   282    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(3-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′-]bipyridinyl-3′-ylmethyl)-propionamide-   283    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   284    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-ethyl]-propionamide-   285    N-(4-cyano-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   287    2-(4-ethanesulfonylamino-3-fluoro-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   288    2-(4-(N,N-dimethylsulfamoylamino)-3-fluorphenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   289    2-(4-methylsulfonamido-3-methoxy-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   290    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenylamino-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   291    N-(2-cyclohexyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   292    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   293    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-thiopropionamide-   294    N-(2-cyclohexylsulfanyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   295    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   296    N-(2-azepan-1-yl-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   297    N-(6-tert-butyl-2-dipropylamino-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   298    N-(2-but-2-enyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   299    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-2-enyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   300    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   301    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   302    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-4-methyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   303    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[2-(4-fluoro-phenyl)-ethyl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide-   304    N-(4-acetyl-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   307    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(phenyl-propionyl-amino)-6″-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide-   308    N-[2-(4-dimethylamino-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   309    2-[3-fluoro-4-(propan-2-sulfonylamino)-phenyl]-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   310    2-[3-fluoro-4-(2,2,2-trifluor-ethansulfonylamino)-phenyl]-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   311    N-[2-(2,6-dimethyl-morpholin-4-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   312    2-(3-fluoro-4-trifluormethylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   313    2-(3-fluoro-4-(sulfamoylamino)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   314    N-[2-(1,1-dioxo-1,6-thiomorpholin-4-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   315    N-(6′-difluormethyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   316    N-(4,6′-dimethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   317    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   318    N-(4,4′-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   319    N-[2-(4-cyclohexyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   320    N-(4′-tert-butyl-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   321    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4′-methoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-propionamide-   322    N-(3′-chloro-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   323    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(3′-fluoro-5-trifluoromethyl-biphenyl-2-ylmethyl)-propionamide-   324    N-(3′-chloro-4′-fluoro-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   325    N-(3′,4′-dimethoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   326    N-[2-(3,4-dimethoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   327    4-(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-yloxymethyl)-piperidine-1-carbonic    acid tert-butyl ester-   328    N-(6-tert-butyl-2-pentyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   329    N-[6-tert-butyl-2-(3-methyl-butoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   330    N-(4-dimethylamino-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   331    N-(2-dipropylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide-   332    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide-   334    N-(2-cyclohex-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   335    N-[2-(1-ethyl-propoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   336    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1-propyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   337    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1-isobutyl-3-methyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   338    N-[2-(4,4-dimethyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   339    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6-trifluoromethyl-2-(4-trifluoromethyl-cyclohexyloxy)-pyridin-3-ylmethyl]-propionamide-   340    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6-trifluoromethyl-2-(4-trifluoromethyl-cyclohexyloxy)-pyridin-3-ylmethyl]-propionamide-   341    4-(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-yloxy)-piperidine-1-carbonic    acid tert-butyl ester-   342    4-[(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-ylamino)-methyl]-piperidine-1-carbonic    acid tert-butyl ester-   343    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(piperidin-4-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   344    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(piperidin-4-yloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   345    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-p-tolyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   346    N-[2-(2-cyclohexyl-vinyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   347    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-butyramide-   348    N-[2-(3,5-dimethoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   349    N-(2-cyclopentyloxy-4-methyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   350    N-(3′,5′-dimethoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   351 ethyl    5-((2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamido)methyl)-6-(4-methylpiperidin-1-yl)-2-(trifluoromethyl)nicotinat    352    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(nonan-5-yloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   353    N-((6-tert-butyl-2-isobutoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   354    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(phenylethynyl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   355    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(3-methoxypropoxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   356    N-((2-(4-benzylpiperidin-1-yl)-4-methyl-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   357    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methylene-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   358    N-[2-(6-aza-spiro[2.5]oct-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   359    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methyl-but-2-enyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   360    N-[2-(3-cyclohexyl-propyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   361    N-[2-(3-ethoxy-propoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   362    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-phenoxy-ethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide-   363    N-[2-(3,5-dimethoxy-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   364    2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-hydroxymethyl-6′-trifluoro    methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide-   365    N-(6′-tert-butyl-4-phenyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   366    N-{6-tert-butyl-2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide-   367    2-(4-methylsulfonamido-3-methyl-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide-   [368]    N-((2-(1H-indol-4-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,-   [369]    N-((6-tert-butyl-2-propoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,-   [370]    N-((6-tert-butyl-2-(3-methoxypropoxy)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,-   [371]    N-((6-tert-butyl-2-(4-(dimethylamino)-4-phenylpiperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,-   [372]    N-((6-tert-butyl-2-methoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,-   [373]    N-((6-tert-butyl-2-ethoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,-   [374]    N-((6-tert-butyl-2-isopropoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,-   [375]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pentyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide,-   [376]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(hexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide,-   [377]    N-((2-(3,5-dimethylcyclohexyloxy)-6-(trifluoromethyl)pyridn-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,-   [378]    N-((6-tert-butyl-2-(2-ethoxyethoxy)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,    in each case optionally in the form of one of the pure stereoisomers    thereof, in particular enantiomers or diastereomers, the racemates    thereof or in the form of a mixture of stereoisomers, in particular    the enantiomers and/or diastereomers, in any desired mixing ratio,    or in each case in the form of corresponding salts or in each case    in the form of corresponding solvates.

Further preferred are the compounds 126, 166, 174, 291, 83, 80, 89, 91,104, 117, 118, 131, 137, 140, 142, 149, 160, 166, 167, 168, 172, 218,235, 127, 196, 256, 257 and 204; still further preferred are thecompounds 126, 166, 174, 291, 83, 80, 89, 91, 104, 117, 118, 131, 137,140, 142, 149, 160, 166, 167, 168, 172, 218 and 235; most preferred arethe compounds 126, 166, 174 and 291.

The present invention accordingly provides compounds of the generalformula I,

in whichX denotes O, S or N—C≡N;n denotes 0, 1, 2, 3 or 4;R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl;Br; I; —SF₅; —NO₂; —CF₃; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹;—C(═O)—OR²²; —C(═O)—R²³; —S(═O)₂—R²⁴ or denote a linear or branched,saturated or unsaturated, unsubstituted or at least monosubstitutedaliphatic C₁₋₁₀ residue;R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)₂—R²⁴;denotes a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;or denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue, optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R^(s)orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁵ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁶ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I;—SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³, —S(═O)₂—R²⁴ or denote a linear or branched,saturated or unsaturated, unsubstituted or at least monosubstitutedaliphatic C₁₋₁₀ residue;R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)₂—R²⁴;denotes a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue and may be fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group;or denotes an unsubstituted or at least monosubstituted 5- to14-membered aryl or heteroaryl residue, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system and/or be attached via a linear orbranched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group;R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)₂—R²⁴ or denotes a linear or branched, saturated or unsaturated,unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue;R¹⁰ denotes —SF_(S); —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹;—C(═O)—OR²²; —C(═O)—R²³; —S(═O)₂—R²⁴;denotes a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀residue, which is in each case substituted with optionally 1, 2, 3, 4,5, 6, 7, 8 or 9 substituents mutually independently selected from thegroup consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃;denotes an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue is in each case attached to the parent structure via acarbon atom in the ring of the cycloaliphatic residue and may be fusedwith a saturated or unsaturated, unsubstituted or at leastmonosubstituted mono- or polycyclic ring system and/or be attached via alinear or branched, unsubstituted or at least monosubstituted C₁₋₆alkylene group;or denotes an unsubstituted or at least monosubstituted 5- to14-membered aryl or heteroaryl residue; which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system and/or be attached via a linear orbranched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group;R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³ and R²⁴,mutually independently, in each casedenote a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;denote an unsaturated or saturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member,which residue may be fused with a saturated or unsaturated,unsubstituted or at least monosubstituted mono- or polycyclic ringsystem and/or be attached via a linear or branched, unsubstituted or atleast monosubstituted C₁₋₆ alkylene group;or denote an unsubstituted or at least monosubstituted 5- to 14-memberedaryl or heteroaryl residue; which may be fused with a saturated orunsaturated, unsubstituted or at least monosubstituted mono- orpolycyclic ring system and/or be attached via a linear or branched,unsubstituted or at least monosubstituted C₁₋₆ alkylene group; orR¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a saturated or unsaturated,unsubstituted or at least monosubstituted 4-, 5-, 6-, 7-, 8- or9-membered heterocycloaliphatic residue, which may be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system; andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue;denote a linear or branched, saturated or unsaturated, unsubstituted orat least monosubstituted aliphatic C₁₋₁₀ residue;or denote an unsaturated or saturated, unsubstituted or at leastmonosubstituted, 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphaticresidue optionally comprising at least one heteroatom as a ring member;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶, together with the carbon atom joining them together as aring member, form a saturated or unsaturated, unsubstituted or at leastmonosubstituted 3-, 4-, 5- or 6-membered cycloaliphatic residue;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Unless otherwise stated, the above-stated aliphatic C₁₋₁₀ residues maypreferably optionally in each case be substituted with 1, 2, 3, 4, 5, 6,7, 8 or 9 substituents mutually independently selected from the groupconsisting of F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C1.5 alkyl),—S(C₁₋₅ alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and—SCF₃.

The above-stated C₁₋₆ alkylene groups may preferably optionally in eachcase be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituentsmutually independently selected from the group consisting of F, Cl, Br,I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅ alkyl), —NH(C₁₋₅alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃.

The above-stated (hetero)cycloaliphatic residues may preferablyoptionally in each case be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of oxo (═O),thioxo (═S), F, Cl, Br, I, —CF₃, —SF₅, —OH, —O—C₁₋₅ alkyl, —NH₂, —NO₂,—O—CF₃, —S—CF₃, —SH, —S—C₁₋₅ alkyl, —C₁₋₅ alkyl, —C(═O)—C₁₋₅ alkyl,—C(═O)—OH, —C(═O)—O—C₁₋₅ alkyl, —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)₂,—O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclicmoiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN,—NO₂, —C₁₋₅ alkyl, —O—C₁₋₅ alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl.

The above-stated (hetero)cycloaliphatic residues may likewise preferablyin each case optionally comprise 1, 2 or 3 (further) heteroatom(s)mutually independently selected from the group consisting of oxygen,nitrogen and sulfur.

The rings of the above-stated mono- or polycyclic ring systems maypreferably optionally in each case be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—C₁₋₅ alkyl, —C₁₋₅ alkyl,—C(═O)—C₁₋₅ alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅ alkyl, —NH(C₁₋₅ alkyl),—N(C₁₋₅ alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein ineach case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyland benzyl may be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, —C₁₋₅ alkyl, —O—C₁₋₅ alkyl, —O—CF₃, —S—CF₃,phenyl and —O-benzyl.

The rings of the above-stated mono- or polycyclic ring systems arepreferably in each case 5-, 6- or 7-membered and may in each caseoptionally comprise 1, 2, 3, 4 or 5 heteroatom(s) as ring member(s),which are mutually independently selected from the group consisting ofoxygen, nitrogen and sulfur.

The above-stated aryl or heteroaryl residues may likewise preferablyoptionally in each case be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of F, Cl, Br,I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅ alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—C₁₋₅ alkyl, alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅ alkyl, —NH(C₁₋₅ alkyl),—N(C₁₋₅ alkyl)₂, —NH—C(═O)—O—C₁₋₅ alkyl, —C(═O)—H, —C(═O)—C_(1-s) alkyl,—C(═O)—NH₂, —C(═O)—NH—C₁₋₅ alkyl, —C(═O)—N—(C₁₋₅ alkyl)₂, —O-phenyl,—O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety ofthe residues —O-phenyl, —O-benzyl, phenyl and benzyl may be substitutedwith 1, 2, 3, 4 or 5 substituents mutually independently selected fromthe group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅alkyl, —O—C₁₋₅ alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl.

The above-stated heteroaryl residues likewise preferably in each caseoptionally comprise 1, 2, 3, 4 or 5 heteroatom(s) mutually independentlyselected from the group consisting of oxygen, nitrogen and sulfur asring member(s).

If one or more of the above-stated residues denotes a saturated orunsaturated C₁₋₁₀ aliphatic residue, i.e. a C₁₋₁₀ alkyl, C₂₋₁₀ alkenylor C₂₋₁₀ alkynyl residue, the latter may preferably be substituted withoptionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, I, —CN,—NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C1.5 alkyl), —NH(C₁₋₅ alkyl),—N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃. C₂₋₁₀ alkenyl residuescomprise at least one, preferably 1, 2, 3 or 4 C—C double bonds andC₂₋₁₀ alkynyl residues comprise at least one, preferably 1, 2, 3 or 4C—C triple bonds.

alkyl residues are preferably selected from the group consisting ofmethyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, n-pentyl, sec-pentyl, neopentyl, n-hexyl and n-heptyl, whichmay optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9substituents mutually independently selected from the group consistingof F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—OCF₃ and —SCF₃.alkenyl residues which are likewise preferred are those selected fromthe group consisting of vinyl, 1-propenyl, 2-propenyl, 1-butenyl,2-butenyl, 3-butenyl, 2-methyl-2-butenyl, 1-pentenyl, 2-pentenyl,3-pentenyl and 4-pentenyl, which may optionally be substituted with 1, 2or 3 substituents mutually independently selected from the groupconsisting of F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—OCF₃ and —SCF₃.

Alkynyl residues which are furthermore preferred are those selected fromthe group consisting of ethynyl, 1-propynyl, 2-propynyl, 1-butynyl,2-butynyl, 3-butynyl, 1-pentynyl, 2-pentynyl, 3-pentynyl and 4-pentynyl,which may optionally be substituted with 1, 2 or 3 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, I, —CN,—NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —OCF₃ and —SCF₃.

Particularly preferred optionally substituted C₁₋₁₀ aliphatic residuesare those selected from the group consisting of methyl, —CF₃, —CHF₂,—CH₂F, —CF₂Cl, —CCl₂F, —CCl₃, —CBr₃, —CH₂—CN, —CH₂—O—CH₃, —CH₂—O—CF₃,—CH₂—SF₃, —CH₂—NH₂, —CH₂—OH, —CH₂—SH, —CH₂—NH—CH₃, —CH₂—N(CH₃)₂,—CH₂—N(C₂H₅)₂, —CH₂—N(CH₃)(C₂H₅), ethyl, —CF₂—CH₃, —CHF—CF₂Cl,—CF₂—CFCl₂, —CFCl—CF₂Cl, —CFCl—CFCl₂, —CH₂—CH₂—NH₂, —CH₂—CH₂—OH,—CH₂—CH₂—SH, —CH₂—CH₂—NH—CH₃, —CH₂—CH₂—N(CH₃)₂, —CH₂—CH₂—N(C₂H₅)₂,—CH₂—CH₂—N(CH₃)(C₂H₅), —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃,—CH₂—CH₂—CN, n-propyl, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—SH,—CH₂—CH₂—CH₂—NH₂, —CH₂—CH₂—CH₂—NH—CH₃, —CH₂—CH₂—CH₂—N(CH₃)₂,—CH₂—CH₂—CH₂—N(C₂H₅)₂, —CH₂—CH₂—CH₂—N(CH₃)(C₂H₅), —CH₂—CH₂—O—CH₃,—CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, —CH₂—CH₂—CH₂—CN, —CH₂—O—CH₂—CH₃,—CH₂—CH₂—SF₃, —CH₂—CH₂—OCF₃, —CH(CH₃)(O—CH₃), —CH(CH₃)(S—CH₃), n-butyl,—CF₂—CF₂—CF₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CN, sec-butyl, isobutyl, tert-butyl,n-pentyl, sec-pentyl, neopentyl, n-hexyl, vinyl, 1-propenyl, 2-propenyl,1-butenyl, 2-butenyl, 3-butenyl, 2-methyl-2-butenyl,(1,1,2)-trifluoro-1-butenyl, 1-pentenyl, 2-pentenyl, 3-pentenyl,4-pentenyl, —CF═CF₂, —CCl═CCl₂, —CH₂—CF═CF₂, —CH₂—CCl═CCl₂, —C≡C—I,—C≡C—F and —C≡C—CI.

If one or more of the above-stated substituents denotes a(hetero)cycloaliphatic residue, which may optionally be fused with asaturated or unsaturated, unsubstituted or at least monosubstitutedmono- or polycyclic ring system, the latter may preferably be selectedfrom the group consisting of cyclopropyl, cyclobutyl, cyclopentyl,cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, cycloheptenyl,imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl,piperidinyl, morpholinyl, piperazinyl, thiomorpholinyl,tetrahydropyranyl, azepanyl, azocanyl, diazepanyl, dithiolanyl,(1,3,4,5)-tetrahydropyrido[4,3-b]indolyl,(3,4)-dihydro-1H-isoquinolinyl, (1,3,4,9)-tetrahydro-[b]-carbolinyl and(1,3)-thiazolidinyl.

The (hetero)cycloaliphatic residues may particularly preferablyoptionally in each case be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of oxo (═O),thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues —O-phenyl, —O-benzyl, phenyl and benzyl may be substituted with1, 2, 3, 4 or 5 substituents mutually independently selected from thegroup consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,—O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and—O-benzyl.

If one or more of the above-stated substituents denotes an aryl residue,the latter may preferably be selected from the group consisting ofphenyl and naphthyl (1-naphthyl and 2-naphthyl).

If one or more of the above-stated substituents denotes a heteroarylresidue, the latter may preferably be selected from the group consistingof thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl,triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, benzo[b]furanyl,benzo[b]thiophenyl, benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl,isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl,quinoxalinyl, quinolinyl and isoquinolinyl.

The aryl or heteroaryl residues may particularly preferably optionallyin each case be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃,—C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein ineach case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyland benzyl may be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, —C₁₋₅ alkyl, —O—C₁₋₅ alkyl, —O—CF₃, —S—CF₃,phenyl and —O-benzyl.

For the purposes of the present invention, a mono- or polycyclic ringsystem is taken to comprise mono- or polycyclic hydrocarbon residueswhich may be saturated or unsaturated and may optionally comprise 1, 2,3, 4 or 5 heteroatom(s) as ring member(s), which are mutuallyindependently selected from the group consisting of oxygen, nitrogen andsulfur.

Such a mono- or polycyclic ring system may, for example, be fused(anellated) with an aryl residue or a heteroaryl residue.

If a polycyclic ring system, such as for example a bicyclic ring system,is present, the various rings may in each case mutually independently beof a different degree of saturation, i.e. be saturated or unsaturated. Apolycyclic ring system is preferably a bicyclic ring system.

(1,3)-benzodioxolyl and (1,4)-benzodioxanyl may be mentioned by way ofexample of aryl residues which are fused with a mono- or polycyclic ringsystem.

If one or more of the above-stated substituents comprises a mono- orpolycyclic ring system, the latter may preferably be substituted with 1,2, 3, 4 or 5 substituents mutually independently selected from the groupconsisting of oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH,—O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃,—SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃,—C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein ineach case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyland benzyl may be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of F, Cl, Br, —OH,—CF₃, —SF₅, —CN, —NO₂, —C₁₋₅ alkyl, —O—C₁₋₅ alkyl, —O—CF₃, —S—CF₃,phenyl and —O-benzyl.

If one or more of the above-stated substituents comprises a linear orbranched C₁₋₆ alkylene group, the latter may preferably be selected fromthe group consisting of —(CH₂)—, —(CH₂)₂—, —C(H)(CH₃)—, —(CH₂)₃—,—(CH₂)₄—, —(CH₂)₅—, —C(H)(C(H)(CH₃)₂)— and —C(C₂H₅)(H)—.

Preferred substituted compounds are those of the above-stated generalformula I, in which

X denotes O, S or N—C≡N;n denotes 0, 1, 2, 3 or 4;R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl;Br; I; —SF₅; —NO₂; —CF₃; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁵; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³; —S(═O)₂—R²⁴ or denote an alkyl residue selectedfrom the group consisting of methyl, ethyl, n-propyl, isopropyl,tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl andn-heptyl;R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁵; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)₂—R²⁴;denotes an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, n-hexyl and n-heptyl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl,cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichis in each case attached to the parent structure via a carbon atom ofthe rings of the above-stated residues and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of oxo (═O), thioxo (═S), F, Cl, Br,I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂,—NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂,—C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —O-phenyl, —O-benzyl, phenyl andbenzyl, wherein in each case the cyclic moiety of the residues—O-phenyl, —O-benzyl, phenyl and benzyl may be substituted with 1, 2, 3,4 or 5 substituents mutually independently selected from the groupconsisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷, mutually independently in each case denote H; F; Cl; Br; I;—SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;—C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³, —S(═O)₂—R²⁴ or denote an alkyl residue selectedfrom the group consisting of methyl, ethyl, n-propyl, isopropyl,tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl andn-heptyl;R⁸ denotes H; F; Cl; Br; I; —SF₅; —CF₃; —CF₂CI; —NO₂; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³;—S(═O)₂—R²⁴;denotes an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, n-hexyl and n-heptyl;denotes an alkenyl residue selected from the group consisting ofethenyl, propenyl, butenyl and pentenyl;denotes an alkynyl residue selected from the group consisting ofethynyl, propynyl, butynyl and pentynyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl,cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichis in each case attached to the parent structure via a carbon atom ofthe rings of the above-stated residues and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of oxo (═O), thioxo (═S), F, Cl, Br,I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂,—NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂,—C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —O-phenyl, —O-benzyl, phenyl andbenzyl, wherein in each case the cyclic moiety of the residues—O-phenyl, —O-benzyl, phenyl and benzyl may be substituted with 1, 2, 3,4 or 5 substituents mutually independently selected from the groupconsisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;or denotes a residue selected from the group consisting of phenyl,naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl,pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl,imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl,benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl,pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, quinoxalinyl, quinolinyland isoquinolinyl, which may in each case be attached via a—(CH₂)—,—(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally besubstituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH,—C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclicmoiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN,—NO₂, —Cl_(—)5 alkyl, —O—C₁₋₅ alkyl, —O—CF₃, —S—CF₃, phenyl and—O-benzyl;R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH;—SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H;—S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶;—C(═O)—NR¹⁷R¹⁹; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³;S(═O)₂—R²⁴ or denotes an alkyl residue selected from the groupconsisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl,sec-butyl, isobutyl, n-pentyl, n-hexyl and n-heptyl;R¹⁰ denotes —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹;—C(═O)—OR²²; —C(═O)—R²³; —S(═O)₂—R²⁴;denotes an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, n-hexyl and n-heptyl which is in each case substituted withoptionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutuallyindependently selected from the group consisting of —CN, —NO₂, —OH,—NH₂, —SH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂,—N(C₂H₅)₂, —N(CH₃)(C₂H₅), —OCF₃ and —SCF₃;denotes an alkenyl residue selected from the group consisting ofethenyl, propenyl, butenyl and pentenyl;denotes an alkynyl residue selected from the group consisting ofethynyl, propynyl, butynyl and pentynyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl,cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichis in each case attached to the parent structure via a carbon atom ofthe rings of the above-stated residues and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of oxo (═O), thioxo (═S), F, Cl, Br,I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂,—NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂,—C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —O-phenyl, —O-benzyl, phenyl andbenzyl, wherein in each case the cyclic moiety of the residues—O-phenyl, —O-benzyl, phenyl and benzyl may be substituted with 1, 2, 3,4 or 5 substituents mutually independently selected from the groupconsisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;or denotes a residue selected from the group consisting of phenyl,naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl,pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl,imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl,benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl,pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, quinoxalinyl, quinolinyland isoquinolinyl, wherein the residue may in each case be attached viaa —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionallybe substituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH,—C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclicmoiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN,—NO₂, —C₁₋₅ alkyl, —O—C₁₋₅ alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³ and R²⁴,mutually independently, in each casedenote an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, n-hexyl and n-heptyl;denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl,cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichmay in each case be attached via a —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or may optionally be substituted with 1, 2, 3, 4 or 5 substituentsmutually independently selected from the group consisting of oxo (═O),thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —O-phenyl, —O-benzyl,phenyl and benzyl, wherein in each case the cyclic moiety of theresidues —O-phenyl, —O-benzyl, phenyl and benzyl may be substituted with1, 2, 3, 4 or 5 substituents mutually independently selected from thegroup consisting of F, Cl, Br, —OH, —CF₃, —SF5, —CN, —NO₂, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,—O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and—O-benzyl;or denote a residue selected from the group consisting of phenyl,naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl,pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl,imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl,benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl,pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, quinoxalinyl, quinolinyland isoquinolinyl, which may in each case be attached via a —(CH₂)—,—(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally besubstituted with 1, 2, 3, 4 or 5 substituents selected from the groupconsisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH,—C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂,—C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂,—O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclicmoiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN,—NO₂, —C₁₋₅ alkyl, —O—C₁₋₅ alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;orR¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of pyrrolidinyl, piperidinyl,(1,3,4,5)-tetrahydropyrido[4,3-b]indolyl,(3,4)-dihydro-1H-isoquinolinyl, (1,3,4,9)-tetrahydro-[b]-carbolinyl,imidazolidinyl, (1,3)-thiazolidinyl, piperazinyl, morpholinyl, azepanyl,diazepanyl and thiomorpholinyl, which may optionally in each case besubstituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of oxo (═O), thioxo (═S), F, Cl, Br,I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂,—NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃,methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂,—C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃,—N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(O₂H₅), —O-phenyl, —O-benzyl, phenyl andbenzyl, wherein in each case the cyclic moiety of the residues—O-phenyl, —O-benzyl, phenyl and benzyl may be substituted with 1, 2, 3,4 or 5 substituents mutually independently selected from the groupconsisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl;andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue;denote an alkyl residue selected from the group consisting of methyl,ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl,n-pentyl, n-hexyl and n-heptyl;or denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶, in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl,cyclopentenyl and cyclohexenyl;whereinunless otherwise stated, the above-stated alkyl, alkenyl and alkynylresidues may in each case optionally be substituted with 1, 2, 3, 4, 5,6, 7, 8 or 9 substituents mutually independently selected from the groupconsisting of F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅,—O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃,—NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅),—OCF₃ and —SCF₃;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise preferred compounds are those of the above-stated generalformula I, in which

X denotes O, S or N—C≡N;n denotes 0, 1, 2, 3 or 4;R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl;Br; I; —SF_(S); —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —S(═O)₂—R²⁴ or denote a residue selected from the groupconsisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F,ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,—CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl,sec-butyl, isobutyl and tert-butyl;R⁵ denotes F; Cl; Br; I; —SF₅; —OR¹⁴; —SR¹⁵; —S(═O)₂—R²⁴;denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CH₂—CN, —CH₂—O—CH₃,—CH₂—O—CF₃, —CH₂—SF₃, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃,—CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, —CH₂—CH₂—CN, n-propyl,—CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, —CH₂—CH₂—CH₂—CN, —CH₂—O—CH₂—CH₃,—CH₂—CH₂—SF₃, —CH₂—CH₂—OCF₃, —CH(CH₃)(O—CH₃), —CH(CH₃)(S—CH₃), n-butyl,—CF₂—CF₂—CF₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CN, sec-butyl, isobutyl andtert-butyl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl,which may optionally in each case be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof oxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,and n-pentyl;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷, mutually independently in each case denote H; F; Cl; Br; I;—SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH;—C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;—S(═O)₂—R²⁴ or denote a residue selected from the group consisting ofmethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,—CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl,—CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl,isobutyl and tert-butyl;R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂;—S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹;—NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—OR²²; —S(═O)₂—R²⁴or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl,tert-butyl, n-pentyl, sec-pentyl, neopentyl, n-hexyl, ethenyl, propenyl,butenyl, pentenyl, ethynyl, propynyl, butynyl, pentynyl, —CF═CF₂,—CCl═Cl₂, —CH₂—CF═CF₂, —CH₂—CCl═CCl₂, —C≡C—F and —C≡C—CI;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichis in each case attached to the parent structure via a carbon atom ofthe rings of the above-stated residues and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of oxo (═O), thioxo (═S), —OH,—O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl,triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl,oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl,quinoxalinyl, quinolinyl and isoquinolinyl, which may in each case beattached via a —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each casemay optionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃,—C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl;R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂;—S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹;—NR¹²R¹³; —OR¹⁴; —SR¹⁵; —S(═O)₂—R²⁴ or denotes a residue selected fromthe group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F,—CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃,—CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,isopropyl, sec-butyl, isobutyl and tert-butyl;R¹⁰ denotes —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂;—C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—OR²²; —S(═O)₂—R²⁴or denotes a residue selected from the group consisting of ethenyl,propenyl, butenyl, pentenyl, ethynyl, propynyl, butynyl, pentynyl,—CF═CF₂, —CCl═Cl₂, —CH₂—CF═CF₂, —CH₂—CCl═CCl₂, —C≡C—I, —C≡C—F and—C≡C—Cl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichis in each case attached to the parent structure via a carbon atom ofthe rings of the above-stated residues and may optionally in each casebe substituted with 1, 2, 3, 4 or 5 substituents mutually independentlyselected from the group consisting of oxo (═O), thioxo (═S), —OH,—O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅,—C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅,—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃;or denotes a residue selected from the group consisting of phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl,triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl,oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl,quinoxalinyl, quinolinyl and isoquinolinyl, which may in each case beattached via a—(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case mayoptionally be substituted with 1, 2, 3, 4 or 5 substituents selectedfrom the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃,—O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,—S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂,—C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂,—N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—C(═O)—O—O₂H₅, —NH—C(═O)—O—C(CH₃)₃,—C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃,—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂,—C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl;R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R²² and R²⁴, mutually independently, in eachcasedenote a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CH₂—CN, —CH₂—O—CH₃,—CH₂—O—CF₃, —CH₂—SF₃, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃,—CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, —CH₂—CH₂—CN, n-propyl,—CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, —CH₂—CH₂—CH₂—CN, —CH₂—O—CH₂—CH₃,—CH₂—CH₂—SF₃, —CH₂—CH₂—OCF₃, —CH(CH₃)(O—CH₃), —CH(CH₃)(S—CH₃), n-butyl,—CF₂—CF₂—CF₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CN, sec-butyl, isobutyl andtert-butyl;denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl,tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl,piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, whichin each case may optionally be substituted with 1, 2, 3, 4 or 5substituents mutually independently selected from the group consistingof oxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl,n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃,—C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and—C(═O)—O—C(CH₃)₃;or denote a residue selected from the group consisting of phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl,triazolyl, pyridinyl, imidazolyl, thiazolyl, oxazolyl and isoxazolyl,wherein the residue may in each case be attached via a —(CH₂)—, —(CH₂)₂—or —(CH₂)₃-group and/or in each case may optionally be substituted with1, 2, 3, 4 or 5 substituents selected from the group consisting of F,Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂,—O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅,—S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl,sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃,—C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅,—NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃,—NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H, —C(═O)—CH₃,—C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂, —C(═O)—NH—CH₃,—C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl,phenyl and benzyl; orR¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which may optionally in eachcase be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of oxo (═O), thioxo(═S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃,—SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl,—C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue;denote an alkyl residue selected from the group consisting of methyl,ethyl and n-propyl;or denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶, in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Further preferred compounds are those of the above-stated generalformula I, in which

X denotes O, S or N—C≡N;n denotes 0, 1 or 2;

R¹, R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br;or denote a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl and —CFCl—CF₂Cl;

R² denotes F; Cl; Br; I or denotes a residue selected from the groupconsisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F,ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,—CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl,sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—CF₃, —O—CCl₃, —O—CBr₃,—O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—C₂H₅, —O—CF₂—CH₃, —O—CH₂—CF₃,—O—C₂H₅, —O—CH₂—CCl₃, —O—CH₂—CBr₃, —O—CHF—CF₂Cl, —O—CF₂—CF₂Cl,—O—CFCl—CF₂Cl, —O—CH₂—CH₂—CH₃, —O—CF₂—CF₂—CF₃, —O—CF(CF₃)₂, —O—CH(CH₃)₂,—O—C(CH₃)₃, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F,—S—CF₂Cl, —S—CCl₂F, —S—C₂H₅, —S—CF₂—CH₃, —S—CH₂—CF₃, —S—C₂F₅,—S—CH₂—CCl₃, —S—CH₂—CBr₃, —S—CHF—CF₂Cl, —S—CF₂—CF₂Cl, —S—CFCl—CF₂Cl,—S—CH₂—CH₂—CH₃, —S—CF₂—CF₂—CF₃, —S—CF(CF₃)₂, —S—CH(CH₃)₂ and —S—C(CH₃)₃;

R⁵ denotes F; Cl; Br; I; —SF₅;denotes a residue selected from the group consisting of —CF₃, —CCl₃,—CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅,—CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, —CF₂—CF₂—CF₃,—CF(CF₃)₂, sec-butyl, isobutyl, tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃,—O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —O—CH₂—CF₃, —O—C₂F₅,—O—CH₂—CCl₃, —O—CH₂—CBr₃, —O—CHF—CF₂Cl, —O—CF₂—CF₂Cl, —O—CFCl—CF₂Cl,—O—CF₂—CF₂—CF₃, —O—CF(CF₃)₂, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CF₃, —S—CCl₃,—S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S—CH₂—CF₃,—S—C₂F₅, —S—CH₂—CCl₃, —S—CH₂—CBr₃, —S—CHF—CF₂Cl, —S—CF₂—CF₂Cl,—S—CFCl—CF₂Cl, —S—CF₂—CF₂—CF₃, —S—CF(CF₃)₂, —S—CH(CH₃)₂, —S—C(CH₃)₃,—S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F,—S(═O)₂—CF₂Cl, —S(═O)₂—CCl₂F, —S(═O)₂—CF₂—CH₃, —S(═O)₂—CH₂—CF₃,—S(═O)₂—C₂F₅, —S(═O)₂—CH₂—CCl₃, —S(═O)₂—CH₂—CBr₃, —S(═O)₂—CHF—CF₂Cl,—S(═O)₂—CF₂—CF₂Cl, —S(═O)₂—CFCl—CF₂Cl, —S(═O)₂—CF₂—CF₂—CF₃,—S(═O)₂—CF(CF₃)₂, —S(═O)₂—CH(CH₃)₂ and —S(═O)₂—C(CH₃)₃;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R¹⁰;R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I;—NO₂; —CN; or denote a residue selected from the group consisting ofmethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,n-propyl, isopropyl, sec-butyl, isobutyl and tert-butyl;R⁸ denotes F; Cl; Br; I; —OH; —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—OR²²;or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl andtert-butyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues;or denotes a residue selected from the group consisting of phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which in each case may optionally be substitutedwith 1, 2, 3, 4 or 5 substituents selected from the group consisting ofF, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃,—SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R⁹ denotes H; F; Cl; Br; I; —NO₂; —CN; or denotes a residue selectedfrom the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CCl₂F, ethyl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl andtert-butyl;R¹⁰ denotes —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;—C(═O)—OR²²;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl;or denotes a residue selected from the group consisting of phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which in each case may optionally be substitutedwith 1, 2, 3, 4 or 5 substituents selected from the group consisting ofF, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃,—SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²², mutually independently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl;or denote a residue selected from the group consisting of phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, wherein theresidue in each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, I, —CN,—CF₃, —SF₅, —OH, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃,—S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl,n-butyl, sec-butyl, isobutyl and tert-butyl; orR¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, which may optionally in eachcase be substituted with 1, 2, 3, 4 or 5 substituents mutuallyindependently selected from the group consisting of oxo (═O), thioxo(═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl,tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂,—C(═O)—C(CH₃)₃, andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue or denote an alkyl residue selected from the group consisting ofmethyl, ethyl and n-propyl;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶, in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those of the above-stated generalformula I, in which

X denotes O or S;n denotes 0, 1 or 2;R¹, R³ and R⁴ in each case denote H;R² denotes F; Cl; Br; I or denotes a residue selected from the groupconsisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃,—O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃,—S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F;R⁵ denotes F; Cl; Br; I; —SF₅;denotes a residue selected from the group consisting of —CF₃, —CCl₃,—CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, tert-butyl, —O—CF₃, —O—CCl₃,—O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —S—CF₃,—S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃,—S(═O)₂—CCl₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ orT denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ orT denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotesC—R′°;R⁶ and R⁷ in each case denote H; F; Cl; Br and I;R⁸ denotes F; Cl; Br; I; —OH; —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵; —C(═O)—OR²²;or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅,—CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃,—CF(CF₃)₂, isopropyl, sec-butyl, isobutyl and tert-butyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues;or denotes a residue selected from the group consisting of phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which in each case may optionally be substitutedwith 1, 2, 3, 4 or 5 substituents selected from the group consisting ofF, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R⁹ denotes H; F; Cl; Br or I;R¹⁰ denotes —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;—C(═O)—OR²²;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues;or denotes a residue selected from the group consisting of phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which in each case may optionally be substitutedwith 1, 2, 3, 4 or 5 substituents selected from the group consisting ofF, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²², mutually independently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl;or denote a residue selected from the group consisting of phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, wherein theresidue in each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, —O—CH₃,—O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,isobutyl and tert-butyl; orR¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, andR²⁵ and R²⁶, mutually independently, in each case denote a hydrogenresidue or denote an alkyl residue selected from the group consisting ofmethyl, ethyl and n-propyl;providing that R²⁵ and R²⁶ do not in each case denote a hydrogenresidue; orR²⁵ and R²⁶, in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Particularly preferred compounds are those the above-stated generalformula I, in which

X denotes O;n denotes 1;R¹, R³ and R⁴ in each case denote H;R² denotes F; Cl; Br or I;R⁵ denotes a residue selected from the group consisting of —CF₃, —CCl₃,—CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, tert-butyl, —O—CF₃, —O—CCl₃,—O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂ and—S—CH₂F;T denotes CH and U denotes CH and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes N and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes CH and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes N and V denotes CH and W denotes C—R⁸ orT denotes N and U denotes CH and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes N and V denotes N and W denotes C—R⁸ orT denotes CH and U denotes CH and V denotes CH and W denotes C—R¹⁵;R⁸ denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴;—SR¹⁵;or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl andtert-butyl;or denotes a residue selected from the group consisting of phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which in each case may optionally be substitutedwith 1, 2, 3, 4 or 5 substituents selected from the group consisting ofF, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂,—O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl,ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R¹⁰ denotes —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵;or denotes a residue selected from the group consisting of phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which in each case may optionally be substitutedwith 1, 2, 3, 4 or 5 substituents selected from the group consisting ofF, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃,—SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl,isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R¹¹, R¹², R¹³, R¹⁴ and R¹⁵, mutually independently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl; orR¹² and R¹³, in each case together with the nitrogen atom joining themtogether as a ring member, form a residue selected from the groupconsisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl, andR²⁵ denotes an alkyl residue selected from the group consisting ofmethyl, ethyl and n-propyl;R²⁶ denotes a hydrogen residue; orR²⁵ and R²⁶, in each case together with the carbon atom joining themtogether as a ring member, form a residue selected from the groupconsisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Very particularly preferred compounds are those of the general formulaIa,

in whichX^(a) denotes O or S;na denotes 0, 1 or 2;R^(2a) denotes F; Cl; Br; I or denotes a residue selected from the groupconsisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃,—O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃,—S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F;R^(5a) denotes F; Cl; Br; I; —SF₅;denotes a residue selected from the group consisting of —CF₃, —CCl₃,—CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, tert-butyl, —O—CF₃, —O—CCl₃,—O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —S—CF₃,—S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃,—S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F and—S(═O)₂—CF₂Cl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;R^(8a) denotes F; Cl; Br; I; —OH; —CN; —NH₂; —NO₂; —NHR^(11a);—NR^(12a)R^(13a); —OR^(14a); —SR^(15a); —C(═O)—OR^(22a);or denotes a residue selected from the group consisting of methyl, —CF₃,—CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃,—C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl,n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl andtert-butyl;denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues;or denotes a residue selected from the group consisting of phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which in each case may optionally be substitutedwith 1, 2, 3, 4 or 5 substituents selected from the group consisting ofF, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11a), R^(12a), R^(13a), R^(14a), R^(15a) and R^(22a), mutuallyindependently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl;or denote a residue selected from the group consisting of phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, wherein theresidue in each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, —O—CH₃,—O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,isobutyl and tert-butyl; orR^(12a) and R^(13a), in each case together with the nitrogen atomjoining them together as a ring member, form a residue selected from thegroup consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise very particularly preferred compounds are those of the generalformula Ib,

in whichnb denotes 0, 1 or 2;R^(2b) denotes F; Cl; Br or I;R^(8b) denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11b);—NR^(12b)R^(13b); —OR^(14b); —SR^(18b);

-   -   denotes a residue selected from the group consisting of methyl,        —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,        —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,        —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,        isopropyl, sec-butyl, isobutyl and tert-butyl;    -   or denotes a residue selected from the group consisting of        phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,        thiophenyl, furanyl and pyridinyl, which in each case may        optionally be substituted with 1, 2, 3, 4 or 5 substituents        selected from the group consisting of F, Cl, Br, I, —CN, —CF₃,        —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,        —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,        n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;        R^(11b), R^(12b), R^(13b), R^(14b), and R^(15b), mutually        independently, in each case    -   denote a residue selected from the group consisting of methyl,        ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;    -   or denote a residue selected from the group consisting of        cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl;        or        R^(12b) and R^(13b), in each case together with the nitrogen        atom joining them together as a ring member, form a residue        selected from the group consisting of pyrrolidinyl, piperidinyl,        piperazinyl, morpholinyl, azepanyl, diazepanyl and        thiomorpholinyl;        in each case optionally in the form of one of the pure        stereoisomers thereof, in particular enantiomers or        diastereomers, the racemates thereof or in the form of a mixture        of stereoisomers, in particular the enantiomers and/or        diastereomers, in any desired mixing ratio, or in each case in        the form of corresponding salts or in each case in the form of        corresponding solvates.

Further very particularly preferred compounds are those of the generalformula Ib,

in whichnb denotes 1;R^(2b) denotes F;R^(8b) denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11b);—NR^(12b)R^(13b); —OR^(14b); —SR^(15b);

-   -   denotes a residue selected from the group consisting of methyl,        —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,        —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,        —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,        isopropyl, sec-butyl, isobutyl and tert-butyl;    -   or denotes a residue selected from the group consisting of        phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,        thiophenyl, furanyl and pyridinyl, which in each case may        optionally be substituted with 1, 2, 3, 4 or 5 substituents        selected from the group consisting of F, Cl, Br, I, —CN, —CF₃,        —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,        —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,        n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;        R^(11b), R^(12b), R^(13b), R^(14b) and R^(15b), mutually        independently, in each case    -   denote a residue selected from the group consisting of methyl,        ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;    -   or denote a residue selected from the group consisting of        cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; or    -   R^(12b) and R^(13b), in each case together with the nitrogen        atom joining them together as a ring member, form a residue        selected from the group consisting of pyrrolidinyl, piperidinyl,        piperazinyl, morpholinyl, azepanyl, diazepanyl and        thiomorpholinyl;        in each case optionally in the form of one of the pure        stereoisomers thereof, in particular enantiomers or        diastereomers, the racemates thereof or in the form of a mixture        of stereoisomers, in particular the enantiomers and/or        diastereomers, in any desired mixing ratio, or in each case in        the form of corresponding salts or in each case in the form of        corresponding solvates.

Further very particularly preferred compounds are those of the generalformula Ic,

in whichnc denotes 0, 1 or 2;R^(2c) denotes F; Cl; Br or I;R^(8c) denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR—NR^(12c)R^(13c);—OR^(14c); —SR^(15c);

-   -   denotes a residue selected from the group consisting of methyl,        —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CCl₂F, ethyl, —CF₂—CH₃,        —OH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl,        n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl,        isobutyl and tert-butyl;    -   or denotes a residue selected from the group consisting of        phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,        thiophenyl, furanyl and pyridinyl, which in each case may        optionally be substituted with 1, 2, 3, 4 or 5 substituents        selected from the group consisting of F, Cl, Br, I, —CN, —CF₃,        —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,        —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,        n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;        R^(11c), R^(12c), R^(13c), R^(14c) and R^(15c), mutually        independently, in each case    -   denote a residue selected from the group consisting of methyl,        ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;    -   or denote a residue selected from the group consisting of        cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; or        R^(12c) and R^(13c), in each case together with the nitrogen        atom joining them together as a ring member, form a residue        selected from the group consisting of pyrrolidinyl, piperidinyl,        piperazinyl, morpholinyl, azepanyl, diazepanyl and        thiomorpholinyl;        in each case optionally in the form of one of the pure        stereoisomers thereof, in particular enantiomers or        diastereomers, the racemates thereof or in the form of a mixture        of stereoisomers, in particular the enantiomers and/or        diastereomers, in any desired mixing ratio, or in each case in        the form of corresponding salts or in each case in the form of        corresponding solvates.

Further very particularly preferred compounds are those of the generalformula Ic,

in whichnc denotes 1;R^(2c) denotes F;R^(8c) denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11c);—NR^(12c)R^(13c); —OR^(14c); —SR^(15c);

-   -   denotes a residue selected from the group consisting of methyl,        —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,        —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,        —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,        isopropyl, sec-butyl, isobutyl and tert-butyl;    -   or denotes a residue selected from the group consisting of        phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,        thiophenyl, furanyl and pyridinyl, which in each case may        optionally be substituted with 1, 2, 3, 4 or 5 substituents        selected from the group consisting of F, Cl, Br, I, —CN, —CF₃,        —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,        —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,        n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;        R^(11c), R^(12c), R^(13c), R^(14c) and R^(15c), mutually        independently, in each case    -   denote a residue selected from the group consisting of methyl,        ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;    -   or denote a residue selected from the group consisting of        cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; or        R^(12c) and R^(13c), in each case together with the nitrogen        atom joining them together as a ring member, form a residue        selected from the group consisting of pyrrolidinyl, piperidinyl,        piperazinyl, morpholinyl, azepanyl, diazepanyl and        thiomorpholinyl;        in each case optionally in the form of one of the pure        stereoisomers thereof, in particular enantiomers or        diastereomers, the racemates thereof or in the form of a mixture        of stereoisomers, in particular the enantiomers and/or        diastereomers, in any desired mixing ratio, or in each case in        the form of corresponding salts or in each case in the form of        corresponding solvates.

Very particularly preferred compounds are those of the general formulaId,

in whichX^(d) denotes O or S;nd denotes 0, 1 or 2;R^(2d) denotes F; Cl; Br; I or denotes a residue selected from the groupconsisting of methyl, —CF₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃,—O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CBr₃, —S—CHF₂, —S—CH₂F,—S—CF₂Cl and —S—CCl₂F;R^(5d) denotes F; Cl; Br; I; —SF₅;denotes a residue selected from the group consisting of —CF₃, —CBr₃,—CHF₂, —CH₂F, —CCl₂F, tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂,—O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃,—S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃,—S(═O)₂—CCl₃, —S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F and—S(═O)₂—CF₂Cl;or denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl;R^(10d) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11d); —NR^(12d)R^(13d);—OR^(14d); —SR^(15d); —C(═O)—OR^(22d);denotes a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl,morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl andthiomorpholinyl, which is in each case attached to the parent structurevia a carbon atom of the rings of the above-stated residues;or denotes a residue selected from the group consisting of phenyl,naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl,furanyl and pyridinyl, which in each case may optionally be substitutedwith 1, 2, 3, 4 or 5 substituents selected from the group consisting ofF, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃,—S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;R^(11d), R^(12d), R^(13d), R^(14d), R^(15d), and R^(22d), mutuallyindependently, in each casedenote a residue selected from the group consisting of methyl, ethyl,n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl;denote a residue selected from the group consisting of cyclopropyl,cyclobutyl, cyclopentyl and cyclohexyl;or denote a residue selected from the group consisting of phenyl,naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, wherein theresidue in each case may optionally be substituted with 1, 2, 3, 4 or 5substituents selected from the group consisting of F, Cl, Br, —O—CH₃,—O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl,isobutyl and tert-butyl; orR^(12d) and R^(13d), in each case together with the nitrogen atomjoining them together as a ring member, form a residue selected from thegroup consisting of pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl,azepanyl, diazepanyl and thiomorpholinyl;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise very particularly preferred compounds are those of the generalformula Ie,

in whichne denotes 0, 1 or 2;R^(2e) denotes F; Cl; Br or I;R^(10e) denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11e);—NR^(12e)R^(13e); —OR^(14e); —SR^(15e);

-   -   denotes a residue selected from the group consisting of methyl,        —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,        —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,        —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,        isopropyl, sec-butyl, isobutyl and tert-butyl;    -   or denotes a residue selected from the group consisting of        phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,        thiophenyl, furanyl and pyridinyl, which in each case may        optionally be substituted with 1, 2, 3, 4 or 5 substituents        selected from the group consisting of F, Cl, Br, I, —CN, —CF₃,        —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,        —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,        n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;        R^(11e), R^(12e), R^(13e), R^(14e) and R^(15e), mutually        independently, in each case    -   denote a residue selected from the group consisting of methyl,        ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;    -   or denote a residue selected from the group consisting of        cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; or        R^(12e) and R^(13e), in each case together with the nitrogen        atom joining them together as a ring member, form a residue        selected from the group consisting of pyrrolidinyl, piperidinyl,        piperazinyl, morpholinyl, azepanyl, diazepanyl and        thiomorpholinyl;        in each case optionally in the form of one of the pure        stereoisomers thereof, in particular enantiomers or        diastereomers, the racemates thereof or in the form of a mixture        of stereoisomers, in particular the enantiomers and/or        diastereomers, in any desired mixing ratio, or in each case in        the form of corresponding salts or in each case in the form of        corresponding solvates.

Likewise very particularly preferred compounds are those of the generalformula Ie,

in whichne denotes 1;R^(2e) denotes F;R^(10e) denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11e);—NR^(12e)R^(13e); —OR^(14e); —SR^(15e);

-   -   denotes a residue selected from the group consisting of methyl,        —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,        —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,        —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,        isopropyl, sec-butyl, isobutyl and tert-butyl;    -   or denotes a residue selected from the group consisting of        phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,        thiophenyl, furanyl and pyridinyl, which in each case may        optionally be substituted with 1, 2, 3, 4 or 5 substituents        selected from the group consisting of F, Cl, Br, I, —CN, —CF₃,        —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,        —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,        n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;        R^(11e), R^(12e), R^(13e), R^(14e) and R^(15e), mutually        independently, in each case    -   denote a residue selected from the group consisting of methyl,        ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;    -   or denote a residue selected from the group consisting of        cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; or        R^(12e) and R^(13e), in each case together with the nitrogen        atom joining them together as a ring member, form a residue        selected from the group consisting of pyrrolidinyl, piperidinyl,        piperazinyl, morpholinyl, azepanyl, diazepanyl and        thiomorpholinyl;        in each case optionally in the form of one of the pure        stereoisomers thereof, in particular enantiomers or        diastereomers, the racemates thereof or in the form of a mixture        of stereoisomers, in particular the enantiomers and/or        diastereomers, in any desired mixing ratio, or in each case in        the form of corresponding salts or in each case in the form of        corresponding solvates.

Likewise very particularly preferred compounds are those of the generalformula If,

in whichnf denotes 0, 1 or 2;R^(2f) denotes F; Cl; Br or I;R^(8f) denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11f);—NR^(12f)R^(13f); —OR^(14f); —SR^(15f);

-   -   denotes a residue selected from the group consisting of methyl,        —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,        —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,        —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,        isopropyl, sec-butyl, isobutyl and tert-butyl;    -   or denotes a residue selected from the group consisting of        phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,        thiophenyl, furanyl and pyridinyl, which in each case may        optionally be substituted with 1, 2, 3, 4 or 5 substituents        selected from the group consisting of F, Cl, Br, I, —CN, —CF₃,        —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,        —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,        n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;        R^(11f), R^(12f), R^(13f), R^(14f) and R^(15f), mutually        independently, in each case    -   denote a residue selected from the group consisting of methyl,        ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;    -   or denote a residue selected from the group consisting of        cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; or        R^(12f) and R^(13f), in each case together with the nitrogen        atom joining them together as a ring member, form a residue        selected from the group consisting of pyrrolidinyl, piperidinyl,        piperazinyl, morpholinyl, azepanyl, diazepanyl and        thiomorpholinyl;        in each case optionally in the form of one of the pure        stereoisomers thereof, in particular enantiomers or        diastereomers, the racemates thereof or in the form of a mixture        of stereoisomers, in particular the enantiomers and/or        diastereomers, in any desired mixing ratio, or in each case in        the form of corresponding salts or in each case in the form of        corresponding solvates.

Likewise very particularly preferred compounds are those of the generalformula If,

in whichnf denotes 1;R^(2f) denotes F;R^(8f) denotes F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11f);—NR^(12f)R^(13f); —OR^(14f); —SR^(15f);

-   -   denotes a residue selected from the group consisting of methyl,        —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl,        —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl,        —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂,        isopropyl, sec-butyl, isobutyl and tert-butyl;    -   or denotes a residue selected from the group consisting of        phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl,        thiophenyl, furanyl and pyridinyl, which in each case may        optionally be substituted with 1, 2, 3, 4 or 5 substituents        selected from the group consisting of F, Cl, Br, I, —CN, —CF₃,        —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH,        —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl,        n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;        R^(11f), R^(12f), R^(13f), R^(14f) and R^(15f), mutually        independently, in each case    -   denote a residue selected from the group consisting of methyl,        ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and        tert-butyl;    -   or denote a residue selected from the group consisting of        cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; or        R^(12f) and R^(13f), in each case together with the nitrogen        atom joining them together as a ring member, form a residue        selected from the group consisting of pyrrolidinyl, piperidinyl,        piperazinyl, morpholinyl, azepanyl, diazepanyl and        thiomorpholinyl;        in each case optionally in the form of one of the pure        stereoisomers thereof, in particular enantiomers or        diastereomers, the racemates thereof or in the form of a mixture        of stereoisomers, in particular the enantiomers and/or        diastereomers, in any desired mixing ratio, or in each case in        the form of corresponding salts or in each case in the form of        corresponding solvates.

Further very particularly preferred compounds are those of the generalformula Ig,

in whichng denotes 0, 1 or 2;R^(2g) denotes F; Cl; Br or I;T denotes CH and U denotes N and V denotes CH orT denotes N and U denotes CH and V denotes CH orT denotes N and U denotes N and V denotes CH orT denotes N and U denotes CH and V denotes N orT denotes CH and U denotes N and V denotes N;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Likewise very particularly preferred compounds are those of the generalformula Ig,

in whichng denotes 1;R^(2g) denotes F;T denotes CH and U denotes N and V denotes CH orT denotes N and U denotes CH and V denotes CH orT denotes N and U denotes N and V denotes CH orT denotes N and U denotes CH and V denotes N orT denotes CH and U denotes N and V denotes N;in each case optionally in the form of one of the pure stereoisomersthereof, in particular enantiomers or diastereomers, the racematesthereof or in the form of a mixture of stereoisomers, in particular theenantiomers and/or diastereomers, in any desired mixing ratio, or ineach case in the form of corresponding salts or in each case in the formof corresponding solvates.

Still further preferred compounds of the above-stated general formula Iare those selected from the group consisting of

-   [1]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-methyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [2]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [3]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [4]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-fluoro-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [5]    N-((2-chloro-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [6]    N-((2-bromo-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [7]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-iodo-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [8]    N-((2-tert-butyl-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [9]    N-((2-cyano-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [10]    (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [11]    (R)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [12]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-morpholino-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [13]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [14]    N-((2-(dimethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [15]    N-((2-(diethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [16]    N-((2-(dipropylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [17]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-hydroxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [18]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-methoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [19]    N-((2-butoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [20]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-isopropoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [21]    N-((2-cyclopentyloxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [22]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-phenyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [23]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(4-fluorophenyl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [24]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((6-(trifluoromethyl)-2,2′-bipyridin-3-yl)methyl)propanamide-   [25]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((6-(trifluoromethyl)-2,3′-bipyridin-3-yl)methyl)propanamide-   [26]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pyrimidin-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [27]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(thiazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [28]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(oxazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [29]    N-((2-(1H-imidazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [30]    N-(2-cyano-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide-   [31]    (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [32]    (R)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [33]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-morpholino-4-(trifluoromethyl)benzyl)propanamide-   [34]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [35]    N-(2-(dimethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [36]    N-(2-(diethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [37]    N-(2-(dipropylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [38]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-hydroxy-4-(trifluoromethyl)benzyl)propanamide-   [39]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-methoxy-4-(trifluoromethyl)benzyl)propanamide-   [40]    N-(2-butoxy-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [41]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-isopropoxy-4-(trifluoromethyl)benzyl)propanamide-   [42]    N-(2-(cyclopentyloxy)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [43]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide-   [44]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((4′-fluoro-5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide-   [45]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-2-yl)-4-(trifluoromethyl)benzyl)propanamide-   [46]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-3-yl)-4-(trifluoromethyl)benzyl)propanamide-   [47]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrimidin-2-yl)-4-(trifluoromethyl)benzyl)propanamide-   [48]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(thiazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide-   [49]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(oxazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide-   [50]    N-(2-(1H-imidazol-2-yl)-4-(trifluoromethypbenzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [51]    N-((6-tert-butyl-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [52]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((4-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [53]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((3-(piperidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide-   [54]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((4-(piperidin-1-yl)-2-(trifluoromethyl)pyrimidin-5-yl)methyl)propanamide-   [55]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((3-(piperidin-1-yl)-5-(trifluoromethyl)pyrazin-2-yl)methyl)propanamide-   [56]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((4-(piperidin-1-yl)-6-(trifluoromethyl)pyridazinyl-3-yl)methyl)propanamide-   [57]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)propanamide-   [58]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperidin-1-yl)-4-(trifluoromethyl)phenyl)propanamide-   [59]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)ethyl)propanamide-   [60]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenethyl)propanamide-   [61]    N-(2-amino-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide-   [62]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-nitro-4-(trifluoromethyl)-benzyl)propanamide-   [63]    N-(4-tert-butyl-2-(piperidin-1-yl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide-   [64]    2-(3-chloro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [65]    2-(3-chloro-4-(methylsulfonamido)phenyl)-N-((2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [66]    2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [67]    2-(3-bromo-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [68]    2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [69]    2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide-   [70]    N-(4-tert-butyl-2-cyanobenzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide-   [71]    N-((6-(chlorodifluoromethyl)-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-(4-methylsulfonamido)phenyl)propanamide-   [72]    (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-morpholino-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [73]    N-((2-(4-benzylpiperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [74]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide;-   [75]    N-(2-chloro-4-(trifluoromethypbenzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [76]    N-((2-(cyclohexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl-2-(3-fluoro-4-methylsulfonamido)phenyl)propanamide-   [77]    N-((3-chloro-5-(trifluoromethyl)pyridin-2-yl)methyl-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [78]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N4(3-(pyrrolidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide-   [79]    N-((2-(3,5-dimethylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [80]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide-   [81]    N-((2-(azepan-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide-   [82]    2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(4-methylpiperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide;    in each case optionally in the form of one of the pure stereoisomers    thereof, in particular enantiomers or diastereomers, the racemates    thereof or in the form of a mixture of stereoisomers, in particular    the enantiomers and/or diastereomers, in any desired mixing ratio,    or in each case in the form of corresponding salts or in each case    in the form of corresponding solvates.

Further preferred compounds of the general formulae A and I according tothe invention are those which, in an FLIPR assay with CHO-K1 cells whichhave been transfected with the human gene VR1, in a concentration ofless than 2000 nM, preferably of less than 1000 nM, particularlypreferably of less then 300 nM, very particularly preferably of lessthan 100 nM, still more preferably of less than 70 nM, still even morepreferably less than 50 nM, most preferably less than 10 nM, effect 50%displacement of capsaicin which is present in a concentration of 100 nM.

In this FLIPR assay, the influx of Ca²⁺ is quantified with theassistance of a Ca²⁺-sensitive dye (type Fluo-4, Molecular Probes EuropeBV, Leiden, Netherlands) in a Fluorescent Imaging Plate Reader (FLIPR,Molecular Devices, Sunnyvale, USA) as described below.

The present invention also provides a process for production ofcompounds of the above-stated general formula I, in accordance withwhich at least one compound of the general formula II,

in which R⁵, U, T, V and W have the above-stated meaning, m denotes 0,1, 2 or 3 and R denotes hydrogen or denotes a C₁₋₆ alkyl residue, isreacted in a reaction medium, in the presence of at least one reducingagent, preferably in the presence of at least one reducing agentselected from the group consisting of sodium hydride, sodium, potassiumhydride, lithium aluminum hydride, sodium borohydride, BH₃xTHF anddi(isobutyl)aluminum hydrideto yield at least one compound of the general formula III,

in which R⁵, U, T, V and W have the above-stated meaning and m denotes0, 1, 2 or 3, and said compound is optionally purified and/or isolated,and at least one compound of the general formula III is reacted in areaction medium in the presence of diphenylphosphoryl azide or in thepresence of HN₃ to yield at least one compound of the general formulaIV,

in which R⁵, U, T, V and W have the above-stated meaning and m denotes0, 1, 2 or 3, and said compound is optionally purified and/or isolated,and at least one compound of the general formula IV is reacted in areaction medium in the presence of at least one reducing agent,preferably in the presence of at least one reducing agent selected fromthe group consisting of sodium hydride, potassium hydride, lithiumaluminum hydride, sodium borohydride and di(isobutyl)aluminum hydrideor in a reaction medium in the presence of a catalyst, preferably in thepresence of a catalyst is based on platinum or palladium, particularlypreferably in the presence of palladium on carbon, and in the presenceof hydrogen or in the presence of hydrazineor in a reaction medium in the presence of triphenylphosphineto yield at least one compound of the general formula V,

in which R⁵, U, T, V and W have the above-stated meaning and m denotes0, 1, 2 or 3, and said compound is optionally purified and/or isolated,or at least one compound of the general formula VI,

in which R⁵, U, T, V, and W have the above-stated meaning and m denotes0, 1, 2 or 3, is reacted in a reaction medium in the presence of atleast one catalyst, preferably in the presence of at least one catalystbased on palladium or platinum, particularly preferably in the presenceof palladium on carbon, optionally in the presence of at least one acid,preferably in the presence of hydrochloric acid, to yield at least onecompound of the general formula V, optionally in the form of acorresponding salt, preferably in the form of a correspondinghydrochloride, and said compound is optionally purified and/or isolated,and at least one compound of the general formula V is reacted with atleast one compound of the general formula VII,

in which R¹, R², R³, R⁴, R²⁵ and R²⁶ have the above-stated meaning, in areaction medium, optionally in the presence of at least one suitablecoupling agent, optionally in the presence of at least one base,or with at least one compound of the general formula VIII,

in which R¹, R², R³, R⁴, V<R²⁵ and R²⁶ have the above-stated meaning andLG denotes a leaving group, preferably a chlorine or bromine atom, in areaction medium, optionally in the presence of at least one base, toyield at least one compound of the general formula Ih,

in which T, U, V, W, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have theabove-stated meaning and n denotes 1, 2, 3 or 4, and said compound isoptionally purified and/or isolated,and optionally at least one compound of the general formula Ih isreacted in a reaction medium with at least one compound of the generalformula IX,

in which the phenyl residues are in each case substituted with 1 or 2substituents mutually independently selected from the group consistingof methoxy, phenoxy, Cl, methyl and Br, preferably in each case with aphenoxy residue or methoxy residue, particularly preferably in each casewith a methoxy residue in para position, or with phosphoruspentasulfide, to yield at least one compound of the general formula Ik,

in which T, U, V, W, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have theabove-stated meaning and n denotes 1, 2, 3 or 4, and said compound isoptionally purified and/or isolated.

The present invention also provides a process for production ofcompounds of the above-stated general formula I, in accordance withwhich at least one compound of the general formula X,

in which R⁵, U, T, V, and W have the above-stated meaning, is reactedwith at least one compound of the general formula VII,

in which R¹, R², R³, R⁴, R²⁵ and R²⁶ have the above-stated meaning, in areaction medium, optionally in the presence of at least one suitablecoupling agent, optionally in the presence of at least one base,or with at least one compound of the general formula VIII,

in which R¹, R², R³, R⁴, R²⁵ and R²⁶ have the above-stated meaning andLG denotes a leaving group, preferably a chlorine or bromine atom, in areaction medium, optionally in the presence of at least one base, toyield at least one compound of the general formula Im,

in which T, U, V, W, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have the above-statedmeaning and said compound is optionally purified and/or isolated,and optionally at least one compound of the general formula Im isreacted in a reaction medium with at least one compound of the generalformula IX,

in which the phenyl residues are in each case substituted with 1 or 2substituents mutually independently selected from the group consistingof methoxy, phenoxy, Cl, methyl and Br, preferably in each case with aphenoxy residue or methoxy residue, particularly preferably in each casewith a methoxy residue in para position, or with phosphoruspentasulfide, to yield at least one compound of the general formula In,

in which T, U, V, W, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have theabove-stated meaning and said compound is optionally purified and/orisolated.

The reaction of compounds of the above-stated general formulae V or Xwith carboxylic acids of the above-stated general formula VII to yieldcompounds of the above-stated general formulae Ih or Im, respectively,preferably proceeds in a reaction medium selected from the groupconsisting of diethyl ether, tetrahydrofuran, acetonitrile, methanol,ethanol, (1,2)-dichloroethane, dimethylformamide, dichloromethane andcorresponding mixtures, optionally in the presence of at least onecoupling reagent, preferably selected from the group consisting of1-benzotriazolyloxy-tris-(dimethyl-amino)-phosphoniumhexafluorophosphate (BOP), dicyclohexylcarbodiimide (DCC),N′-(3-dimethylaminopropyl)-N-ethylcarbodiimide (EDCI),diisopropylcarbodiimide, 1,1′-carbonyl-diimidazole (CDI),N-[(dimethylamino)-1H-1,2,3-triazolo-[4,5-b]-pyridino-1-ylmethylene]-N-methylmethaneaminiumhexafluorophosphate N-oxide (HATU),O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate(HBTU), O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluroniumtetrafluorborate (TBTU) and 1-hydroxy-7-azabenzotriazole (HOAt),optionally in the presence of at least one organic base, preferablyselected from the group consisting of triethylamine, pyridine,dimethylaminopyridine, N-methylmorpholine and diisopropylethylamine,preferably at temperatures of −70° C. to 100° C.

Alternatively, the reaction of compounds of the above-stated generalformulae V or X with carboxylic acid derivatives of the above-statedgeneral formula VIII, in which LG denotes a leaving group, preferably achlorine or bromine atom, to yield compounds of the above-stated generalformulae Ih or Im proceeds in a reaction medium which is preferablyselected from the group consisting of diethyl ether, tetrahydrofuran,acetonitrile, methanol, ethanol, dimethylformamide, dichloromethane andcorresponding mixtures, optionally in the presence of an organic orinorganic base, preferably selected from the group consisting oftriethylamine, dimethylaminopyridine, pyridine and diisopropylamine, attemperatures of −70° C. to 100° C.

The reaction of compounds of the general formulae Ih or Im to yieldcompounds of the general formulae Ik or In preferably proceeds in areaction medium selected from the group consisting of toluene,para-xylene, ortho-xylene, meta-xylene, acetonitrile, dichloromethane,dimethylformamide and mixtures of the above-stated reaction media, withaddition of a dithiaphosphetane, particularly preferably with additionof 2,4-bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-disulfide(Lawesson's reagent), or with addition of phosphorus pentasulfide, attemperatures of 50 to 150° C.

The compounds of the above-stated formulae I, II, Ill, IV, V, VI, VIII,IX and X are in each case commercially obtainable and may also beproduced using conventional methods known to the person skilled in theart.

The synthesis method for compounds of the general formula VII may befound in the document “4-(methylsulfonylamino)phenyl analogues asvanilloid antagonist showing excellent analgesic activity and thepharmaceutical compositions comprising the same” of J. W. Lee et al. [WO2005/003084-A1]. The corresponding parts of the reference are herebydeemed to be part of the disclosure.

The above-described reactions may in each case be performed under theconventional conditions familiar to the person skilled in the art, forexample with regard to pressure or the sequence of addition of thecomponents. Optimum control of the process may optionally be establishedby the person skilled in the art by simple preliminary testing. Theintermediate and final products obtained by the above-describedreactions may in each case, if desired and/or necessary, be purifiedand/or isolated by conventional methods known to the person skilled inthe art. Suitable purification methods are, for example, extractionmethods and chromatographic methods such as column chromatography orpreparative chromatography. All the above-described process steps and ineach case also the purification and/or isolation of intermediate orfinal products may be performed in part or entirely under an inert gasatmosphere, preferably under a nitrogen atmosphere.

Those compounds of the above-stated general formulae I, Ia, Ia1, Ib,Ib1, Ic, Ic1, Id, Id1, Ie, Ie1, If, If1, Ig, Ih, Ik, Im, In, A, B1, B2,C1 and C2 in form of their (S)-enantiomer may be preferred. The(S)-enantiomer of compounds of general formula Ia is given by way ofexample.

The substituted compounds according to the invention of the above-statedgeneral formulae I, Ia, Ia1, Ib, Ib1, Ic, Ic1, Id, Id1, Ie, Ie1, If,If1, Ig, Ih, Ik, Im, In, A, B1, B2, C1 and C2, hereinafter designatedonly as compounds of the general formula I, and correspondingstereoisomers may be isolated both in the form of the free basesthereof, the free acids thereof and in the form of corresponding salts,in particular physiologically acceptable salts.

The free bases of the particular substituted compounds according to theinvention of the above-stated general formula I and correspondingstereoisomers; in particular compounds of the above-stated generalformula I which comprise a pyridinyl moiety or a basic moiety in placeof the substituent R⁸, may, for example, be converted into thecorresponding salts, preferably physiologically acceptable salts byreaction with an inorganic or organic acid, preferably with hydrochloricacid, hydrobromic acid, sulfuric acid, phosphoric acid, methanesulfonicacid, p-toluenesulfonic acid, carbonic acid, formic acid, acetic acid,oxalic acid, succinic acid, tartaric acid, mandelic acid, fumaric acid,lactic acid, citric acid, glutamic acid or aspartic acid. The free basesof the respective substituted compounds of the above-stated generalformula I and corresponding stereoisomers may likewise be converted intothe corresponding physiologically acceptable salts with the free acid ora salt of a sugar substitute, such as for example saccharin, cyclamateor acesulfame.

The free acids of the substituted compounds of the above-stated generalformula I and corresponding stereoisomers may correspondingly beconverted into the corresponding physiologically acceptable salts byreaction with a suitable base. Alkali metal salts, alkaline earth metalsalts or ammonium salts [NH_(x)R_(4-x)]⁺, in which x=0, 1, 2, 3 or 4 andR denotes a linear or branched C₁₋₄ alkyl residue may be mentioned byway of example.

The substituted compounds according to the invention of the above-statedgeneral formula I and corresponding stereoisomers may optionally, likethe corresponding acids, the corresponding bases or salts of thesecompounds, also be obtained in the form of the solvates thereof,preferably in the form of the hydrates thereof, by conventional methodsknown to the person skilled in the art.

If the substituted compounds according to the invention of theabove-stated general formula I are obtained after the production thereofin the form of the stereoisomers thereof, preferably in the form of theracemates thereof or other mixtures of their various enantiomers and/ordiastereomers, these may be separated and optionally isolated byconventional methods known to the person skilled in the art. Exampleswhich may be mentioned are chromatographic separation methods, inparticular liquid chromatography methods at standard pressure or atelevated pressure, preferably MPLC and HPLC methods, and fractionalcrystallization methods. Individual enantiomers, e.g. diastereomericsalts formed by means of HPLC on a chiral stationary phase or by meansof crystallization with chiral acids, such as (+)-tartaric acid,(−)-tartaric acid or (+)-10-camphorsulfonic acid, may here in particularbe separated from one another.

The substituted compounds according to the invention of the above-statedgeneral formula I and corresponding stereoisomers as well as in eachcase the corresponding acids, bases, salts and solvates aretoxicologically safe and are therefore suitable as pharmaceutical activeingredients in pharmaceutical preparations.

The present invention accordingly also provides a pharmaceuticalpreparation containing at least one compound according to the inventionof the above-stated general formula I, in each case optionally in theform of one of the pure stereoisomers thereof, in particular enantiomersor diastereomers, the racemates thereof or in the form of a mixture ofstereoisomers, in particular the enantiomers and/or diastereomers, inany desired mixing ratio, or in each case in the form of a correspondingsalt, or in each case in the form of a corresponding solvate, andoptionally one or more pharmaceutically acceptable auxiliary substances.

These pharmaceutical preparations according to the invention are inparticular suitable for regulating the vanilloid receptor 1 (VR1/TRPV1),preferably for inhibiting the vanilloid receptor 1 (VR1/TRPV1) and/orfor stimulating the vanilloid receptor 1 (VR1/TRPV1).

The pharmaceutical preparations according to the invention are likewisepreferably suitable for prevention and/or treatment of disorders ordiseases which are at least in part mediated by vanilloid receptors 1.

The pharmaceutical preparation according to the invention is preferablysuitable for the treatment and/or prevention of one or more diseasesselected from the group consisting of pain selected from the groupconsisting of acute pain, chronic pain, neuropathic pain and visceralpain; joint pain; hyperalgesia; allodynia; causalgia; migraine;depression; neuropathy; nerve injury; neurodegenerative diseases,preferably selected from the group consisting of multiple sclerosis,Alzheimer's disease, Parkinson's disease and Huntington's chorea;cognitive dysfunction, preferably cognitive deficiency states,particularly preferably memory disorders; epilepsy; airways diseases,preferably selected from the group consisting of asthma, bronchitis andpulmonary inflammation; coughing; urinary incontinence; an overactivebladder (OAB); diseases and/or injuries of the gastrointestinal tract;duodenal ulcers; gastric ulcers; irritable bowel syndrome; strokes; eyeirritation; skin irritation; neurotic skin conditions; allergic skindiseases; psoriasis; vitiligo; herpes simplex; inflammation, preferablyinflammation of the intestines, the eyes, the bladder, the skin or thenasal mucosa; diarrhea; pruritus; osteoporosis; arthritis;osteoarthritis; rheumatic diseases; disorders of food intake, preferablyselected from the group consisting of bulimia, cachexia, anorexia andobesity; dependency on medicines; abuse of medicines; withdrawalsymptoms associated with dependency on medicines; development oftolerance towards medicines, preferably towards natural or syntheticopioids; dependency on drugs; drug abuse; withdrawal symptoms associatedwith dependency on drugs; dependency on alcohol; alcohol abuse andwithdrawal symptoms associated with dependency on alcohol; for diuresis;for antinatriuresis; for influencing the cardiovascular system; forincreasing vigilance; for the treatment of wounds and/or burns; for thetreatment of severed nerves; for increasing libido; for modulatinglocomotor activity; for anxiolysis; for local anaesthesia and/or forinhibiting undesired side-effects, preferably selected from the groupconsisting of hyperthermia, high blood pressure and constriction of thebronchial tubes, triggered by the administration of agonists of thevanilloid receptor 1 (VR1/TRPV1 receptors), preferably selected from thegroup consisting of capsaicin, resiniferatoxin, olvanil, arvanil,SDZ-249665, SDZ-249482, nuvanil and capsavanil.

The pharmaceutical preparation according to the invention isparticularly preferably suitable for the treatment and/or prevention ofone or more diseases selected from the group consisting of pain,preferably of pain selected from the group consisting of acute pain,chronic pain, neuropathic pain and visceral pain; joint pain; migraine;depression; neurodegenerative diseases, preferably selected from thegroup consisting of multiple sclerosis, Alzheimer's disease, Parkinson'sdisease and Huntington's chorea; cognitive dysfunction, preferablycognitive deficiency states, particularly preferably memory disorders;inflammation, preferably inflammation of the intestines, the eyes, thebladder, the skin or the nasal mucosa; urinary incontinence; anoveractive bladder (OAB); dependency on medicines; abuse of medicines;withdrawal symptoms associated with dependency on medicines; developmentof tolerance towards medicines, preferably development of tolerancetowards natural or synthetic opioids; dependency on drugs; drug abuse;withdrawal symptoms associated with dependency on drugs; dependency onalcohol; alcohol abuse and withdrawal symptoms associated withdependency on alcohol.

The pharmaceutical preparation according to the invention is veryparticularly preferably suitable for the treatment and/or prevention ofpain, preferably of pain selected from the group consisting of acutepain, chronic pain, neuropathic pain and visceral pain, and/or urinaryincontinence.

The present invention also provides the use of at least one compoundaccording to the invention and optionally one or more pharmaceuticallyacceptable auxiliary substances for the production of a pharmaceuticalpreparation for regulating the vanilloid receptor 1 (VR1/TRPV1),preferably for inhibiting the vanilloid receptor 1 (VR1/TRPV1) and/orfor stimulating the vanilloid receptor 1 (VR1/TRPV1).

It is preferred to use at least one substituted compound according tothe invention and optionally one or more pharmaceutically acceptableauxiliary substances for the production of a pharmaceutical preparationfor the prevention and/or treatment of disorders or diseases which areat least in part mediated by vanilloid receptors 1.

It is particularly preferred to use at least one compound according tothe invention and optionally one or more pharmaceutically acceptableauxiliary substances for the production of a pharmaceutical preparationfor the treatment and/or prevention of one or more diseases selectedfrom the group consisting of pain, preferably of pain selected from thegroup consisting of acute pain, chronic pain, neuropathic pain andvisceral pain and joint pain.

It is particularly preferred to use at least one compound according tothe invention and optionally one or more pharmaceutically compatibleauxiliary substances for the production of a pharmaceutical preparationfor the treatment and/or prevention of one or more diseases selectedfrom the group consisting of hyperalgesia; allodynia; causalgia;migraine; depression; neuropathy; nerve injury; neurodegenerativediseases, preferably selected from the group consisting of multiplesclerosis, Alzheimer's disease, Parkinson's disease and Huntington'schorea; cognitive dysfunction, preferably cognitive deficiency states,particularly preferably memory disorders; epilepsy; airways diseases,preferably selected from the group consisting of asthma, bronchitis andpulmonary inflammation; coughing; urinary incontinence; an overactivebladder (OAB); diseases and/or injuries of the gastrointestinal tract;duodenal ulcers; gastric ulcers; irritable bowel syndrome; strokes; eyeirritation; skin irritation; neurotic skin conditions; allergic skindiseases; psoriasis; vitiligo; herpes simplex; inflammation, preferablyinflammation of the intestines, the eyes, the bladder, the skin or thenasal mucosa; diarrhea; pruritus; osteoporosis; arthritis;osteoarthritis; rheumatic diseases; disorders of food intake, preferablyselected from the group consisting of bulimia, cachexia, anorexia andobesity; dependency on medicines; abuse of medicines; withdrawalsymptoms associated with dependency on medicines; development oftolerance towards medicines, preferably towards natural or syntheticopioids; dependency on drugs; drug abuse; withdrawal symptoms associatedwith dependency on drugs; dependency on alcohol; alcohol abuse andwithdrawal symptoms associated with dependency on alcohol; for diuresis;for antinatriuresis; for influencing the cardiovascular system; forincreasing vigilance; for the treatment of wounds and/or burns; for thetreatment of severed nerves; for increasing libido; for modulatinglocomotor activity; for anxiolysis; for local anaesthesia and/or forinhibiting undesired side-effects, preferably selected from the groupconsisting of hyperthermia, high blood pressure and constriction of thebronchial tubes, triggered by the administration of agonists of thevanilloid receptor 1 (VR1/TRPV1 receptors), preferably selected from thegroup consisting of capsaicin, resiniferatoxin, olvanil, arvanil,SDZ-249665, SDZ-249482, nuvanil and capsavanil.

It is very particularly preferred to use at least one substitutedcompound according to the invention and optionally one or morepharmaceutically acceptable auxiliary substances for the production of apharmaceutical preparation for the treatment and/or prevention of one ormore diseases selected from the group consisting of pain, preferably ofpain selected from the group consisting of acute pain, chronic pain,neuropathic pain and visceral pain; joint pain; migraine; depression;neurodegenerative diseases, preferably selected from the groupconsisting of multiple sclerosis, Alzheimer's disease, Parkinson'sdisease and Huntington's chorea; cognitive dysfunction, preferablycognitive deficiency states, particularly preferably memory disorders;inflammation, preferably inflammation of the intestines, the eyes, thebladder, the skin or the nasal mucosa; urinary incontinence; anoveractive bladder (OAB); dependency on medicines; abuse of medicines;withdrawal symptoms associated with dependency on medicines; developmentof tolerance towards medicines, preferably development of tolerancetowards natural or synthetic opioids; dependency on drugs; drug abuse;withdrawal symptoms associated with dependency on drugs; dependency onalcohol; alcohol abuse and withdrawal symptoms associated withdependency on alcohol.

It is still further preferred to use at least one substituted compoundaccording to the invention and optionally one or more pharmaceuticallycompatible auxiliary substances for the production of a pharmaceuticalpreparation for the treatment and/or prevention of pain, preferablyselected from the group consisting of acute pain, chronic pain,neuropathic pain and visceral pain, and/or urinary incontinence.

The pharmaceutical preparation according to the invention is suitablefor administration to adults and children including small children andbabies.

The pharmaceutical preparation according to the invention may beformulated as a liquid, semisolid or solid dosage form, for example inthe form of solutions for injection, drops, succi, syrups, sprays,suspensions, tablets, patches, capsules, dressings, suppositories,ointments, creams, lotions, gels, emulsions, aerosols or inmultiparticulate form, for example in the form of pellets or granules,optionally pressed into tablets, packaged in capsules or suspended in aliquid, and may also be administered as such.

In addition to at least one substituted compound of the above-statedgeneral formula I, optionally in the form of one of the purestereoisomers thereof, in particular enantiomers or diastereomers, theracemate thereof or in the form of mixtures of the stereoisomers, inparticular the enantiomers or diastereomers, in any desired mixingratio, or optionally in the form of a corresponding salt or in each casein the form of a corresponding solvate, the pharmaceutical preparationaccording to the invention conventionally contains furtherphysiologically acceptable pharmaceutical auxiliary substances, whichare for example selected from the group consisting of matrix materials,fillers, solvents, diluents, surface-active substances, dyes,preservatives, disintegrants, slip agents, lubricants, aromas andbinders.

Selection of the physiologically acceptable auxiliary substances and thequantities thereof which are to be used depends upon whether thepharmaceutical preparation is to be administered orally, subcutaneously,parenterally, intravenously, intraperitoneally, intradermally,intramuscularly, intranasally, buccally, rectally or topically, forexample onto infections of the skin, mucous membranes or eyes.Preparations in the form of tablets, coated tablets, capsules, granules,pellets, drops, succi and syrups are preferred for oral administration,while solutions, suspensions, readily reconstitutible dried preparationsand sprays are preferred for parenteral, topical and inhalatoryadministration. The substituted compounds according to the inventionused in the pharmaceutical preparation according to the invention in adepot in dissolved form or in a dressing, optionally with the additionof skin penetration promoters, are suitable percutaneous administrationpreparations. Orally or percutaneously administrable formulations mayalso release the particular substituted compound according to theinvention in delayed manner.

Production of the pharmaceutical preparations according to the inventionproceeds with the assistance of conventional means, devices, methods andprocesses known to the person skilled in the art, such as are describedfor example in “Remington's Pharmaceutical Sciences”, ed. A. R. Gennaro,17th ed., Mack Publishing Company, Easton, Pa. (1985), in particular inpart 8, chapters 76 to 93. The corresponding description is herebyintroduced as a reference and is deemed to be part of the disclosure.The quantity of the particular substituted compounds according to theinvention of the above-stated general formula I to be administered tothe patient may vary and is for example dependent on the weight or ageof the patient and on the mode of administration, the indication and theseverity of the complaint. Conventionally, 0.001 to 100 mg/kg,preferably 0.05 to 75 mg/kg, particularly preferably 0.05 to 50 mg/kg ofpatient body weight of at least one such compound according to theinvention are administered.

Pharmacological Methods I. Functional Investigation of the VanilloidReceptor 1 (VR1/TRPV1 Receptor)

The agonistic or antagonistic action of the substances to beinvestigated on the vanilloid receptor 1 (VR1/TRPV1) of the rat speciesmay be determined by the following assay. According to this assay, theinflux of Ca²⁺ through the receptor channel is quantified with theassistance of a Ca²⁺-sensitive dye (type Fluo-4, Molecular Probes EuropeBV, Leiden, Netherlands) in a Fluorescent Imaging Plate Reader (FLIPR,Molecular Devices, Sunnyvale, USA).

Method:

Complete medium: 50 mL HAMS F12 Nutrient Mixture (Gibco Invitrogen GmbH,Karlsruhe, Germany) with

10 vol. % FCS (foetal calf serum, Gibco Invitrogen GmbH, Karlsruhe,Germany, heat-inactivated);

2 mM L-glutamine (Sigma, Munich, Germany);

1 wt. % AA solution (antibiotic/antimycotic solution, PAA, Pasching,Austria) and 25 ng/mL NGF medium (2.5 S, Gibco Invitrogen GmbH,Karlsruhe, Germany)

Cell culture plate: poly-D-lysine coated, black 96 well plates with aclear bottom (96 well black/clear plate, BD Biosciences, Heidelberg,Germany) are additionally coated with laminin (Gibco Invitrogen GmbH,Karlsruhe, Germany), by diluting laminin to a concentration of 100 μg/mLwith PBS (Ca—Mg-free PBS, Gibco Invitrogen GmbH, Karlsruhe, Germany).Aliquots with a concentration of 100 μg/mL of laminin are taken andstored at −20° C. The aliquots are diluted with PBS in a 1:10 ratio to10 μg/mL of laminin and a 50 μL portion is in each case pipetted into awell of the cell culture-plate. The cell culture-plates are incubated at37° C. for at least two hours, the supernatant solution is aspirated andthe wells are in each case washed twice with PBS. The coated cellculture-plates are stored with supernatant PBS, which is not removeduntil just before application of the cells.

Preparation of the Cells:

The spinal column is removed from decapitated rats and is placeddirectly in cold, i.e. located in an ice bath, HBSS buffer (Hank'sbuffered saline solution, Gibco Invitrogen GmbH, Karlsruhe, Germany)combined with 1 vol. % (percent by volume) of an AA solution(antibiotic/antimycotic solution, PAA, Pasching, Austria). The spinalcolumn is cut open longitudinally and removed together with fasciae fromthe spinal canal. The dorsal root ganglia (DRGs) are then removed and inturn stored in cold HBSS buffer combined with 1 vol. % of an AAsolution. The DRGs, from which all traces of blood and spinal nerveshave been removed, are in each case transferred into 500 μL of coldcollagenase type 2 (PAA, Pasching, Austria) and incubated for 35 minutesat 37° C. After addition of 2.5 vol. % of trypsin (PAA, Pasching,Austria), incubation is continued for a further 10 minutes at 37° C.Once incubation is complete, the enzyme solution is carefully removed bypipette and the DRGs, which are left behind, are in each case combinedwith 500 μL of complete medium.

The DRGs are in each case repeatedly suspended, drawn by means of asyringe through no. 1, no. 12 and no. 16 cannulas and transferred into50 mL Falcon microtubes and each tube is made up to 15 mL with completemedium. The contents of each Falcon microtube are in each case filteredthrough a 70 μm Falcon filter insert and centrifuged for 10 minutes at1200 revolutions and room temperature. The resultant pellet is in eachcase resuspended in 250 μL of complete medium and the cell countdetermined.

The number of cells in the suspension is adjusted to 3×10⁵ per mL and a150 μL portion of this suspension is in each case placed in a well ofthe cell culture plate which has been coated as described above. Theplates are placed in an incubator at 37° C., 5 vol. % CO₂ and 95%relative atmospheric humidity for two to three days.

The cells are then loaded with 2 μM Fluo-4 and 0.01 vol. % Pluronic F127(Molecular Probes Europe BV, Leiden, Netherlands) in HBSS buffer (Hank'sbuffered saline solution, Gibco Invitrogen GmbH, Karlsruhe, Germany) for30 min at 37° C., washed 3 x with HBSS buffer and, after a further 15minutes' incubation at room temperature, used for Ca²⁺ measurement inthe FLIPR assay. Ca²⁺-dependent fluorescence is here measured before andafter the addition of substances (λex=488 nm, λem=540 nm).Quantification proceeds by measuring the highest fluorescence intensity(FC, fluorescence counts) over time.

FLIPR Assay:

The FLIPR protocol comprises 2 additions of substance. The compounds tobe tested (10 μM) are firstly pipetted onto the cells and Ca²⁺ influx iscompared with the control (capsaicin 10 μM). This provides thepercentage activation relative to the Ca²⁺ signal after addition of 10μM of capsaicin (CP). After 5 minutes' incubation, 100 nM of capsaicinare added and the influx of Ca²⁺ is again determined.

Desensitising agonists and antagonists result in suppression of Ca²⁺influx. The percentage inhibition in comparison with the maximumachievable inhibition with 10 μM capsaicin is calculated.

Triplicate determinations (n=3) are performed and these are repeated inat least 3 independent experiments (N=4).

On the basis of the percentage displacement by different concentrationsof the compounds to be tested of the general formula I, IC₅₀ inhibitionconcentrations which bring about 50% displacement of capsaicin werecalculated. K, values for the test substances were obtained byconversion using the Cheng-Prusoff equation (Cheng, Prusoff; Biochem.Pharmacopoeia. 22, 3099-3108, 1973).

II. Functional Investigations on the Vanilloid Receptor (VR1)

The agonistic or antagonistic action of the substances to beinvestigated on the vanilloid receptor (VR1) may also be determined withthe following assay. According to this assay, the influx of Ca²⁺ throughthe channel is quantified with the assistance of a Ca²⁺-sensitive dye(type Fluo-4, Molecular Probes Europe BV, Leiden, Netherlands) in aFluorescent Imaging Plate Reader (FLIPR, Molecular Devices, Sunnyvale,USA).

Method:

Chinese hamster ovary cells (CHO K1 cells, European Collection of CellCultures (ECACC), Great Britain) are stably transfected with the VR1gene. For functional investigations, these cells are plated out ontopoly-D-lysine-coated, black 96 well plates with a clear bottom (BDBiosciences, Heidelberg, Germany) at a density of 25,000 cells/well. Thecells are incubated overnight at 37° C. and 5% CO₂ in a culture medium(Ham's Nutrient Mixture F12, 10 vol. % FCS (foetal calf serum), 18 μg/mLL-proline). On the following day, the cells are incubated with Fluo-4(Fluo-4 2 μM, Pluronic F127 0.01 vol. %, Molecular Probes in HBSS(Hank's buffered saline solution), Gibco Invitrogen GmbH, Karlsruhe,Germany) for 30 minutes at 37° C. The plates are then washed 3 timeswith HBSS buffer and, after a further 15 minutes' incubation at roomtemperature, used for Ca²⁺⁻ measurement in the FLIPR. Ca²⁺-dependentfluorescence is here measured before and after addition of thesubstances to be investigated (wavelength λ_(ex)=488 nm, λ_(em)=540 nm).Quantification proceeds by measuring the highest fluorescence intensity(FC, fluorescence counts) over time.

FLIPR Assay:

The FLIPR protocol comprises 2 additions of substance. The substances tobe tested (10 μM) are firstly pipetted onto the cells and Ca²⁺ influx iscompared with the control (capsaicin 10 μM) (% activation relative tothe Ca²⁺ signal after addition of 10 μM of capsaicin). After 5 minutes'incubation, 100 nM of capsaicin are added and the influx of Ca²⁺ isagain determined.

Desensitising agonists and antagonists resulted in suppression of Ca²⁺influx. The percentage inhibition in comparison with the maximumachievable inhibition with 10 μM capsaicin is calculated.

On the basis of the percentage displacement by different concentrationsof the compounds to be tested of the general formula I, IC₅₀ inhibitionconcentrations which bring about 50% displacement of capsaicin werecalculated. K; values for the test substances were obtained byconversion using the Cheng-Prusoff equation (Cheng, Prusoff; Biochem.Pharmacopoeia. 22, 3099-3108, 1973).

III. Formaldehyde Test in Mice

The investigation for determining the antinociceptive action of thecompounds according to the invention is carried out by the formaldehydetest on male mice (NMRI, 20 to 30 g body weight, Iffa, Credo, Belgium).

In the formaldehyde test according to D. Dubuisson et al., Pain, 1977,4, 161-174, a distinction is drawn between the first (early) phase (0-15min after formaldehyde injection) and the second (late) phase (15-60 minafter formaldehyde injection). The early phase, being a direct responseto the formaldehyde injection, is considered to be a model of acutepain, while the late phase is considered to be a model of persistent(chronic) pain (T. J. Corre et al., Pain, 1993, 52, 259-285). Thecorresponding literature descriptions are hereby introduced as areference and are deemed to be part of the disclosure.

The compounds according to the invention are investigated in the secondphase of the formaldehyde test in order to obtain information concerningthe effects of the substances on chronic/inflammatory pain.

The timing of the administration of the compounds according to theinvention prior to the formaldehyde injection is selected as a functionof the mode of administration of the compounds according to theinvention. Intravenous administration of the test substances in anamount of 10 mg/kg of body weight proceeds 5 minutes before theformaldehyde injection. This is achieved by a single, subcutaneousformaldehyde injection (20 μL, 1% aqueous solution) into the dorsal sideof the rear hind paw, such that a nociceptive reaction is induced in thefreely mobile test animals, the reaction being expressed by distinctlicking and biting of the affected paw.

Nociceptive behaviour is then continuously recorded by observing theanimals for a period of three minutes in the second (late) phase of theformaldehyde test (21 to 24 minutes after the formaldehyde injection).Pain behaviour is quantified by summing the seconds for which theanimals exhibit licking and biting of the affected paw over theinvestigation period.

The comparison is made in each case with control animals, which, insteadof compounds according to the invention, received vehicle (0.9% aqueoussodium chloride solution) before administration of the formaldehyde. Onthe basis of the quantification of the pain behaviour, the action of thesubstance in the formaldehyde test is determined as a percentage changerelative to the corresponding control.

After injection of substances which are antinociceptive in theformaldehyde test, the described behaviors of the animals, i.e. lickingand biting, are reduced or eliminated.

IV. Investigation of Analgesic Efficacy by the Writhing Test

Investigation of the compounds according to the invention of the generalformula I for analgesic efficacy was performed by phenylquinone-inducedwrithing in the mouse, modified after I. C. Hendershot and J. Forsaith(1959) J. Pharmacol. Exp. Ther. 125, 237-240. The correspondingliterature description is hereby introduced as a reference and is deemedto be part of the disclosure.

Male NMRI mice weighing from 25 to 30 g were used for this purpose.Groups of 10 animals per compound dose received, 10 minutes afterintravenous administration of the compounds to be tested, 0.3 mL/mouseof a 0.02% aqueous solution of phenylquinone (phenylbenzoquinone, Sigma,Deisenhofen, Germany; solution prepared with addition of 5% of ethanoland stored in a water bath at 45° C.) administered intraperitoneally.The animals were placed individually in observation cages. A push buttoncounter was used to record the number of pain-induced stretchingmovements (writhing reactions=straightening of the torso with stretchingof the rear extremities) for 5-20 minutes after phenylquinoneadministration. The control was provided by animals which had receivedonly physiological saline. All the compounds were tested at the standarddosage of 10 mg/kg.

V. Hypothermie Assay an der Maus

Male NMRI mice (weight 25-35 gram, supplier IFFA CREDO, Bruxelles,Belgium) are used in the hypothermie assay. The animals are kept understandardized conditions: light/darkness interval (6:00 to 18:00 light;18:00 to 6:00 Uhr darkness), room temperature 19-22° C., relativehumidity 35-70%, 15 times per hour change of compartment air, airflow<0.2 m/sec. The animals were fed on a standardized diet (ssniff diet,ssniff Spezialdiäten GmbH, Soest, Germany) and tap water. Water and dietwere detracted during the experiment. All animals were used once in theexperiment. The animals were allowed to adapt to the experimentalconditions for at least 5 days.

The acute application of capsaicin (VR-1 agonist) leads to a decrease ofthe core body temperature in rat and mice via stimulation of heatsensors. Only compounds which act as specific VR-1-receptor antagonistscan antagonize the capsaicin induced hypothermie. In contrast, morphineinduced hypothermie is not antagonized by VR-1 antagonists. Thus, thisexperiment is suitable for the determination of compounds that act asVR1-antagonists via their effect on the core body temperature.

For the determination of the core body temperature a digital thermometerwas used (Thermalert TH-5, physitemp, Clifton N.J., USA). The measuringhead was inserted into the rectum.

The individual basis value is determined by measuring the bodytemperature twice in an interval of about half an hour. Subsequently agroup of mice (n=6 to 10) is treated with capsaicin (3 mg/kg)intraperitoneally (i.p.). Another group of mice (n=6 to 10) is treatedwith capsaicin (3 mg/kg) intraperitoneally (i.p.) and the test compound(i.v. or p.o.). The test compound is given 10 min (i.v.) or 15 min(p.o.), respectively, before application of capsaicin. The bodytemperature is determined 7,5/15 and 30 min after application ofcapsaicin(i.v.+i.p.) or 15/30/60/90/120 min after application ofcapsaicin (p.o.+i.p.), respectively. In addition, another group of miceis only given the test compound or a vehicle control.

The measuring points are given as average values +/−S.E.M. of theabsolute values. The antagonistic effect is given in percent ofinhibition of capsaicin induced hypothermie.

VI. Neuropathic Pain in Mice

The efficacy of compounds of general formula I in the treatment ofneuropathic pain is investigated by using the Bennet modell (chronicconstriction injury; Bennett and Xie, 1988, Pain 33: 87-107.

¹H NMRI mice (weight 16 to 18 g) under ketavet-rompun anaesthesia aresupplied with three loose ligatures of the right nervus ischiaticus. Theanimals develop an oversensitivity to cold at the position of the padthat is innervated by the injured nerve which—after a recovery period ofone week—is quantified over a period of three weeks by using a metalplate that is cooled to 4° C. (cold allodynia). The animals are observedfor a period of 2 minutes on this plate and the number of briskwithdrawal reactions of the injured nerve is counted. The efficacy ofthe compounds is determined at different time points afteradministration of test compound (e.g. 15, 30, 45, and 60 min) relatingto the value before substance application and the resulting area anderthe curve (AUC) and/or blocking of cold allodynia at different timepoints is expressed either in percent efficacy relative to vehiclecontrol (AUC) or relative to the initial value (time points). The groupsize is n=10, the stastical significance of efficacy against allodynia(*=p<0.05) is determined by analysis of variance with repeatedmeasurements and post hoc analysis with Bonferroni adjustment.

The invention is illustrated below with the assistance of some Examples.These explanations are given merely by way of example and do notrestrict the general concept of the invention.

EXAMPLES

The yields of the compounds produced have not been optimised.

All temperatures are uncorrected.

The term “equivalents” means molar equivalents, “RT” means roomtemperature, “M” and “N” are concentrations stated in mol/l, “aq.” meansaqueous, “sat.” means saturated, “soln.” means solution.

Further Abbreviations:

DMF N,N-dimethylformamide

EDCI N-ethyl-N′-(3-dimethylaminopropyl)-carbodiimide hydrochloride

EA ethyl acetate

H₂O water

MeOH methanol

The chemicals and solvents used were purchased from conventionalsuppliers (Acros, Avocado, Aldrich, Bachem, Fluka, Lancaster, Maybridge,Merck, Sigma, TCl, Oakwood etc.) or synthesised by conventional methodsknown to the person skilled in the art.

Silica gel 60 (0.0-0.063 mm) from E. Merck, Darmstadt, was used as thestationary phase for the column chromatography.

Thin-layer chromatography was performed with pre-coated silica gel 60 F254 HPTLC plates from E. Merck, Darmstadt.

The mixture ratios of solvents, mobile solvents or for chromatographicinvestigations are always stated by volume/volume.

Analysis was carried out by mass spectroscopy and NMR.

1. General Method for the Preparation of Amines of the General FormulaV-A

Amines of the general formula V-A are prepared as shown in scheme 1below.

Stage 1: Method A:

Compounds of the general formula VI-A (1 equivalent), in which R⁵, U, Tand V have the above-stated meaning and m denotes 0, 1, 2 or 3, arestirred with an amine of the general formula HNR¹²R¹³ (6 equivalents)for 48 hours at RT. The reaction mixture is combined with 1 Nhydrochloric acid and repeatedly extracted with EA. The aqueous phase issaturated with NaCl and then extracted again with EA. The combinedorganic phases are washed with 1 N hydrochloric acid and with sat. aq.NaCl soln., dried over MgSO₄ and the solvent is removed under a vacuum.

The following compounds A-1 to A-6 were obtained according to theabove-stated general method:

Compound A-1 2-(piperidin-1-yl)-6-(trifluoromethyl)nicotinonitrile

The compound was obtained in a yield of 86% as a pale yellow oil.

¹H NMR (300 MHz, CDCl₃)

7.87 (d, 1H, J=7.8 Hz), 6.95 (d, 1H, J=7.8 Hz), 3.78 (m, 4H), 1.71 (m,6H)

IR (KBr) 2941, 2857, 2218, 1590, 1496, 1453, 1346, 1318, 1239, 1186 cm⁻¹MS (FAB) m/z 256 (M+H)

Compound A-2 2-(morpholin-4-yl)-6-(trifluoromethyl)nicotinonitrile

The compound was obtained in a yield of 78% as a pale yellow oil.

¹H NMR (300 MHz, CDCl₃)

7.94 (d, 1H, J=7.8 Hz), 7.05 (d, 1H, J=7.8 Hz), 3.84 (s, 8H)

IR (KBr) 3397, 2968, 1511, 1428, 1337, 1124 cm⁻¹ MS (FAB) m/z 258 (M+H)

Compound A-3 2-(pyrrolidin-1-yl)-6-(trifluoromethyl)nicotinonitrile

The compound was obtained in a yield of 85% as a pale yellow oil.

¹H NMR (300 MHz, CDCl₃)

7.83 (d, 1H, J=7.8 Hz), 6.86 (d, 1H, J=7.8 Hz), 3.78-3.83 (m, 4H),1.96-2.04 (m, 4H)

IR (KBr) 2976, 2880, 2216, 1591, 1502, 1457, 1344, 1303, 1247, 1181 cm⁻¹MS (FAB) m/z 242 (M+H)

Compound A-4 2-(piperidin-1-yl)-4-(trifluoromethyl)benzonitrile

The compound was obtained in a yield of 74% as a pale yellow oil.

¹H NMR (300 MHz, CDCl₃)

7.63 (d, 1H, J=7.8 Hz), 7.1-7.19 (m, 2H), 3.22-3.26 (m, 4H), 1.60-1.80(m, 6H)

Compound A-5 2-(morpholin-4-yl)-4-(trifluoromethyl)benzonitrile

The compound was obtained in a yield of 80% as a pale yellow oil.

¹H NMR (300 MHz, CDCl₃)

8.31 (d, 1H, J=7.8 Hz), 7.85-7.88 (m, 2H), 4.36-4.39 (m, 4H), 3.76-3.79(m, 4H)

IR (KBr) 2856, 1614, 2210, 1501, 1430, 1311, 1258, 1173, 1122, 1077 cm⁻¹

Compound A-6 2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzonitrile

The compound was obtained in a yield of 80% as a pale yellow oil.

¹H NMR (400 MHz, CDCl₃)

7.53 (d, 1H, J=8.8 Hz), 6.83-6.85 (m, 2H), 3.65 (t, 4H, J=6.4 Hz), 2.04(t, 4H, J=6.4 Hz)

IR (KBr) 2972, 2212, 1619, 1561, 1504, 1454, 1306, 1169 cm⁻¹

Method B:

Compounds of the general formula VI-A (1 equivalent), in which R⁵, U, Tand V have the above-stated meaning and m denotes 0, 1, 2 or 3, arestirred with an amine of the general formula HNR¹²R¹³ (2 equivalents)and DBU [1,8-d]aza-bicyclo[5.4.0]andec-7-ene] (2 equivalents) inacetonitrile (7 mL per mmol of compound of general formula VI-A) for 18hours at RT. The reaction mixture is repeatedly extracted with EA. Thecombined organic extracts are washed with sat. aq. NaCl soln., driedover MgSO₄ and the solvent is removed under a vacuum. The residue ispurified by flash chromatography (SiO₂, different mixtures of hexanesand EA).

The following compounds A-7 to A-102 were obtained according to theabove-stated general method:

Compound A-7:6-(chlorodifluoromethyl)-2-(piperidin-1-yl)pyridine-3-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.87 (d, 1H, J=7.8 Hz), 6.94 (δ, 1H, J=7.8Hz), 3.22-3.26 (m, 4H), 1.60-1.80 (m, 6H); IR (neat) 2939, 2857, 2217,1588, 1493, 1451, 1296, 1235, 1109, 977, 917, 807 cm⁻¹; MS (FAB) m/z 272(M+H)

A-8:2-(4-benzylpiperazin-1-yl)-6-(trifluoromethyl)pyridine-3-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.83 (d, 1H, J=7.8 Hz), 7.19-7.30 (m, 5H),6.94 (d, 1H, J=7.8 Hz), 3.80-3.83 (m, 4H), 3.52 (s, 2H), 2.52-2.56 (m,4H); IR (neat) 2813, 1590, 1498, 1451, 1321, 1239, 1143, 968, 824, 742cm⁻¹; MS (FAB) m/z 347 (M+H)

A-9:6-(trifluoromethyl)-2-(4-methylppiperidin-1-yl)pyridine-3-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.87 (d, 1H, J=7.8 Hz), 6.95 (d, 1H, J=7.8Hz), 4.53 (m, 2H), 3.05 (m, 2H), 1.78 (m, 2H), 1.64 (m, 1H), 1.29 (m,2H), 1.00 (d, 3H, J=6.6 Hz); IR (neat) 2926, 2852, 2218, 1590, 1497,1456, 1324, 1237, 1186, 1147, 1082, 963 cm⁻¹; MS (FAB) m/z 270 (M+H)

A-10:6-(trifluoromethyl)-2-(3,5-dimethylpiperidin-1-yl)pyridine-3-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.84 (d, 1H, J=7.8 Hz), 6.91 (d, 1H, J=7.8Hz), 4.50 (m, 2H), 2.49 (m, 2H), 1.67-1.89 (m, 4H), 0.92 (d, 6H, J=6.6Hz)

IR (neat) 2925, 2852, 2216, 1592, 1498, 1457, 1325, 1188, 1145, 1080,962 cm⁻¹ MS (FAB) m/z 284 (M+H)

A-11: 2-azocan-1-yl-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=7.8 Hz), 6.87 (d, 1H, J=7.8 Hz), 3.88 (t, 4H, J=6.0 Hz),1.87 (m, 4H), 1.55 (m, 4H); IR (KBr) 2929, 2857, 2213, 1592, 1563, 1510,1455, 1327, 1235, 1188, 1145, 1080, 999, 816, 743 cm⁻¹; MS (FAB) m/z284(M+H)

A-12:4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.90 (dd, 1H, J=7.5, 0.9 Hz), 7.20-7.35 (m, 5H), 7.00 (d, 1H, J=7.5 Hz),4.70 (dt, 2H, J=13.5, 1.8 Hz), 3.17 (dt, 2H, J=13.5, 3.3 Hz), 2.82 (m,1H), 1.95 (m, 2H), 1.87 (m, 2H); IR (KBr) 2938, 2852, 2217, 1590, 1566,1376, 1190, 1145, 1081, 1012, 958, 824, 752 cm⁻¹; MS (FAB) m/z 332(M+H)

A-13:4-fluoro-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.93 (dd, 1H, J=7.5, 0.9 Hz), 7.04 (d, 1H,J=7.5 Hz), 4.94 (dm, 1H, J=48.3 Hz), 3.98 (m, 2H), 3.81 (m, 1H),1.90-2.13 (m, 4H) MS (FAB) m/z 274(M+H)

A-14:6′-(chloro-difluoro-methyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.86 (d, 1H, J=7.5 Hz), 6.93 (d, 1H, J=7.5Hz), 4.53 (m, 2H), 3.05 (m, 2H), 1.62-1.80 (m, 3H), 1.23-1.27 (m, 2H),0.99 (d, 3H, J=6.6 Hz); IR (KBr) 2925, 2217, 1589, 1559, 1497, 1455,1336, 12231, cm⁻¹ MS (FAB) m/z 286(M+H)

A-15: 2-azepan-1-yl-6-(chloro-difluoro-methyl)-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.85 (d, 1H, J=7.5 Hz), 6.85 (d, 1H, J=7.5Hz), 3.87 (t, 4H, J=6=Hz), 1.90 (m, 4H), 1.60 (m, 4H); IR (KBr) 2931,2214, 1590, 1558, 1506, 1455, 1339 cm⁻¹; MS (FAB) m/z 286(M+H)

A-16:6′-(4-fluoro-phenyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.00 (m, 2H), 7.77 (d, 1H, J=7.8 Hz),7.07-7.17 (m, 3H), 4.51 (m, 2H), 3.05 (m, 2H), 1.77 (m, 2H), 1.66 (m,1H), 1.35 (m, 2H), 0.99 (d, 3H, J=6.6 Hz); IR (KBr) 2935, 2210, 1576,1508, 1449, 1329, 1233, 1156, 1116, 1021, 949 cm⁻¹; MS (FAB) m/z296(M+H)

A-17: 2-azepan-1-yl-6-(4-fluoro-phenyl)-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.00 (m, 2H), 7.75 (d, 1H, J=7.8 Hz), 7.13(dd, 1H, J=8.7, 8.7 Hz), 7.01 (d, 1H, J=7.8 Hz), 3.92 (t, 4H, J=6=Hz),1.92 (m, 4H), 1.60 (m, 4H); IR (KBr) 2930, 2855, 2206, 1577, 1504, 1452,1338, 1277, 1234, 1155, 848, 805 cm⁻¹; MS (FAB) m/z 296(M+H)

A-18: 6-(chloro-difluoro-methyl)-2-dipropylamino-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.82 (d, 1H, J=7.8 Hz), 6.83 (d, 1H, J=7.8Hz), 3.63 (t, 4H, J=7.5 Hz), 1.73 (m, 4H), 0.96 (t, 6H, J=7.2 Hz); IR(KBr) 2968, 2214, 1590, 1455, 1374, 1232, 1108 cm⁻¹; MS (FAB) m/z288(M+H)

A-19: 2-(1,3-dihydro-isoindol-2-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.93 (d, 1H, J=7.8 Hz), 7.30-7.37 (m, 4H),6.97 (d, 1H, J=7.8 Hz), 5.20 (s, 4H); IR (KBr) 2966, 2213, 1588, 1480,1455, 1374, 1232, 1176 cm⁻¹; MS (FAB) m/z 290(M+H)

A-20:3′-cyano-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-carbonicacid ethylester

¹H NMR (300 MHz, CDCl₃)

8.22 (dd, 1H, J=8.1, 0.6 Hz), 7.90 (d, 1H, J=8.1 Hz), 7.24-7.42 (m, 5H),4.41 (m, 2H), 4.16 (q, 2H, J=7.0 Hz), 3.38 (m, 2H), 2.73 (m, 2H), 2.08(m, 2H), 1.21 (t, 3H, J=7.0 Hz); IR (neat) 2926, 2218, 1725, 1590, 1495,1456, 1321, 1186, 1148, 1040, 963, 824, 738, 698 cm⁻¹; MS (FAB) m/z 404(M+H)

A-21:4,6′-bis-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.94 (d, 1H, J=7.8 Hz), 7.07 (d, 1H, J=7.8 Hz), 4.62 (m, 2H), 3.07 (m,2H), 2.35 (m, 1H), 2.03 (m, 2H), 1.70 (m, 2H)

IR (neat) 2964, 2221, 1591, 1495, 1456, 1394, 1342, 1254, 1147, 1084,960, 827, 744, 697 cm⁻¹; MS (FAB) m/z 324 (M+H)

A-22:4-methoxymethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.88 (d, 1H, J=7.8 Hz), 6.97 (d, 1H, J=7.8 Hz), 4.57 (m, 2H), 3.35 (s,3H), 3.27 (d, 2H, J=6.0 Hz), 3.07 (m, 2H), 1.87 (m, 2H), 1.28-1.45 (m,3H); IR(neat) 2951, 2237, 1590, 1465, 1431, 1349, 1269, 1188, 1150,1117, 969, 842, 743 cm⁻¹; MS (FAB) m/z 300 (M+H)

A-23: 2-(4-p-tolyl-piperazin-1-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.93 (d, 1H, J=7.5 Hz), 7.11 (d, 2H, J=8.4 Hz), 7.05 (d, 1H, J=7.5 Hz),6.88 (d, 2H, J=8.4 Hz), 4.00 (m, 4H), 3.28 (m, 4H), 2.28 (s, 3H); IR(neat) 2918, 2219, 1590, 1513, 1449, 1381, 1319, 1236, 1186, 1147, 1086,1044, 970, 815, 743, 703 cm⁻¹; MS (FAB) m/z 347 (M+H)

A-24: 2-(4-m-tolyl-piperazin-1-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.94 (d, 1H, J=7.8 Hz), 7.19 (t, 1H, J=7.5 Hz), 7.06 (d, 1H, J=7.8 Hz),6.72-6.78 (m, 3H), 4.00 (m, 4H), 3.33 (m, 4H), 2.34 (s, 3H)

IR (neat) 2830, 2214, 1591, 1487, 1320, 1345, 1184, 1140, 1088, 967,816, 770, 694 cm¹; MS (FAB) m/z 347 (M+H)

A-25:2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.93 (d, 1H, J=7.8 Hz), 7.05 (d, 1H, J=7.8 Hz), 6.94 (d, 2H, J=6.9 Hz),6.86 (d, 2H, J=6.9 Hz), 4.00 (m, 4H), 3.77 (s, 3H), 3.21 (m, 4H); IR(neat) 2832, 2219, 1590, 1510, 1448, 1319, 1241, 1184, 1146, 1085, 1035,970, 825, 743, 702 cm⁻¹; MS (FAB) m/z 363 (M+H)

A-26:6-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.96 (d, 1H, J=8.1 Hz), 7.52 (d, 2H, J=8.7 Hz), 7.09 (d, 1H, J=8.1 Hz),6.94 (d, 2H, J=8.7 Hz), 4.01 (m, 4H), 3.46 (m, 4H);

IR(neat) 2923, 2220, 1685, 1594, 1509, 1455, 1344, 1318, 1233, 1186,1147, 1089, 965, 818 cm⁻¹; MS (FAB) m/z 401 (M+H)

A-27:6-trifluoromethyl-2-[4-(3-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.22 (d, 1H, J=3.3 Hz), 7.93 (d, 1H, J=7.5 Hz), 7.63 (d, 1H, J=7.5 Hz),7.06 (d, 1H, J=9.0 Hz), 6.89 (m, 1H), 4.01 (m, 4H), 3.53 (m, 4H); IR(neat) 2856, 2216, 1589, 1441, 1375, 1344, 1312, 1234, 1148, 1097, 1023,969, 832 cm⁻¹; MS (FAB) m/z 402 (M+H)

A-28: 2-imidazol-1-yl-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.62 (s, 1H), 8.38 (d, 1H, J=7.9 Hz), 8.00 (s,1H), 7.76 (d, 1H, J=7.9 Hz), 7.29 (s, 1H); IR (neat) 3132, 2228, 1574,1479, 1440, 1339, 1304, 1245, 1191, 1151, 1102, 1051, 985, 845, 744, 651cm⁻¹; MS (FAB) m/z 239(M-FH)

A-29:2-(4-(3-chloropyridin-2-yl)piperazin-1-yl)-6-(trifluoromethyl)nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.46 (d, 1H, J=4.5 Hz), 7.89-7.95 (m, 2H), 7.04-7.07 (m, 2H), 3.99 (m,4H), 3.44 (m, 4H); IR (neat) 2851, 2212, 1568, 1430, 1363, 1332, 1228,1145, 1105, 962, 851 cm⁻¹; MS (FAB) m/z 372 (M+H)

A-30: 2-(4-cyclohexyl-piperazin-1-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.90 (d, 1H, J=7.8 Hz), 6.98 (d, 1H, J=7.8 Hz), 3.86 (m, 4H), 2.70 (m,4H), 2.31 (m, 1H), 1.80 (m, 4H), 1.20-1.28 (m, 6H); MS (FAB) m/z 339(M+H)

A-31:4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4,3′-dicarbonitrile

¹H NMR (300 MHz, CDCl₃)

7.97 (d, 1H, J=7.8 Hz), 7.33-7.53 (m, 5H), 7.13 (d, 1H, J=7.8 Hz), 4.66(m, 2H), 3.55 (m, 2H), 2.15-2.31 (m, 4H); IR (neat) 2927, 2221, 1590,1494, 1455, 1381, 1320, 1242, 1145, 1084, 1021, 963, 905, 829, 759, 699cm⁻¹; MS (FAB) m/z 357 (M+H)

A-32:4-phenylamino-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.90 (d, 1H, J=7.8 Hz), 7.19 (m, 2H), 7.02 (d,1H, J=7.8 Hz), 6.65 (m, 3H), 4.42 (m, 2H), 3.57 (m, 1H), 3.30 (m, 2H),2.22 (m, 2H), 1.53 (m, 2H); MS (FAB) m/z 347 (M+H)

A-33: 2-azepan-1-yl-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.86 (d, 1H, J=7.1 Hz), 6.88 (d, 1H, J=7.7Hz), 3.84-3.91 (m, 4H), 1.82-1.94 (m, 4H), 1.54-1.64 (m, 4H); IR (neat)2930, 2215, 1593, 1563, 1508, 1458, 1327, 1246, 1144, 817 cm⁻¹; MS (FAB)m/z 270 (M+H)

A-34:N-(3′-cyano-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-yl)-N-phenyl-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.85 (d, 1H, J=7.8 Hz), 7.41 (m, 3H), 7.11 (m,2H), 6.95 (d, 2H, J=7.8 Hz), 4.96 (m, 1H), 4.61 (m, 2H), 3.14 (m, 2H),1.96 (m, 4H), 1.46 (m, 2H), 1.03 (t, 3H, J=7.5 Hz); MS (FAB) m/z403(M+H)

A-35: 2-(4-dimethylamino-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.14 (d, 1H, J=8.1 Hz), 8.04 (d, 2H, J=8.7Hz), 7.52 (d, 1H, J=7.8 Hz), 6.77 (d, 2H, J=8.7 Hz), 3.06 (s, 6H); IR(neat) 2969, 2215, 1571, 1522, 1463, 1409, 1341, 1254, 1132, 1088, 1024,844, 790, 763 cm⁻¹; MS (FAB) m/z 292(M+H)

A-36: 2-(2,6-dimethyl-morpholin-4-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.85 (d, 1H, J=7.5 Hz), 6.97 (d, 1H, J=7.5Hz), 4.31 (m, 2H), 3.68 (m, 2H), 2.74 (m, 2H), 1.19 (d, 6H, J=6.3 Hz);IR (neat) 2979, 2867, 2220, 1591, 1566, 1452, 1330, 1297, 1240, 1146,1080, 1008, 967, 828, 745 cm⁻¹; MS (FAB) m/z 286 (M+H)

A-37: 2-(1,1-dioxo-thiomorpholin-4-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.06 (d, 1H, J=7.5 Hz), 7.27 (d, 1H, J=7.5Hz), 4.32 (m, 4H), 3.23 (m, 4H); IR(neat) 2923, 2223, 1588, 1455, 1334,1179, 1126, 1084, 865, 833 cm⁻¹; MS (FAB) m/z 306 (M+H)

A-38:4,6′-dimethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.60 (d, 1H, J=7.8 Hz), 6.53 (d, 1H, J=7.8Hz), 4.39 (m, 2H), 2.96 (m, 2H), 2.41 (s, 3H), 1.60-1.76 (m, 3H), 1.35(m, 2H), 0.98 (d, 3H, J=6.3 Hz); IR(neat) 2922, 2847, 2211, 1585, 1556,1453, 1375, 1331, 1245, 1105, 965, 808, 764 cm⁻¹; MS (FAB) m/z 216(M+H)

A-39:4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.92 (d, 1H, J=7.8 Hz), 7.33-7.40 (m, 2H), 6.99-7.06 (m, 3H), 6.07 (m,1H), 4.43 (q, 2H, J=3.0 Hz), 4.08 (t, 2H, J=4.8 Hz), 2.72 (q, 2H, J=5.7Hz); IR(neat) 2923, 2220, 1685, 1594, 1509, 1455, 1344, 1318, 1233,1186, 1147, 1089, 965, 818 cm⁻¹; MS (FAB) m/z 348 (M+H)

A-40:4-dimethylamino-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.81 (d, 1H, J=8.1 Hz), 7.32-7.37 (m, 2H), 7.20-7.25 (m, 3H), 6.89 (d,1H, J=8.1 Hz), 4.05 (m, 2H), 3.61 (m, 2H), 2.25 (m, 4H), 2.02 (s, 6H);IR(neat) 2945, 2867, 2784, 2217, 1590, 1497, 1452, 1321, 1240, 1146,1082, 954, 913, 823, 736 cm⁻¹; MS (FAB) m/z 284(M+H)

A-41: 2-(4-methyl-piperidin-1-yl)-4-trifluoromethyl-benzonitrile

IR (neat) 2924, 2223, 1500, 1433, 1319, 1175, 1134, 1080, 1134, 829cm⁻¹; MS (FAB) m/z 269 (M+H)

A-42: 2-butylamino-6-trifluoromethyl-nicotinonitrile

IR (neat) 3359, 2961, 2228, 1602, 1536, 1351, 1277, 1200, 1131, 821cm⁻¹; MS (FAB) m/z 244 (M+H)

A-43: 2,2-dimethyl-propionicacid-3′-cyano-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-ylester

¹H NMR (CDCl₃) δ 7.92 (dd, 1H, J=7.9, 0.8 Hz), 7.04 (d, 1H, J=7.7 Hz),5.09-5.04 (m, 1H), 3.99-3.76 (m, 4H), 2.06-1.80 (m, 4H), 1.22 (s, 9H);IR (neat) 2969, 2232, 1727, 1592, 1459, 1325, 1156, 1029 cm⁻¹

A-44: acetic acid3′-cyano-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-ylester

¹H NMR (CDCl₃) δ 7.92 (dd, 1H, J=7.9, 0.3 Hz), 7.05 (d, 1H, J=7.9 Hz),5.06 (m, 1H), 4.11-4.03 (m, 2H), 3.70-3.62 (m, 2H), 2.10-2.00 (m, 2H),2.09 (s, 3H), 1.87-1.76 (m, 2H); IR (neat) 2959, 2220, 1736, 1591, 1459,1243, 1146, 1029 cm⁻¹

A-45:4-methoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (CDCl₃) δ 7.90 (d, 1H, J=7.9 Hz), 7.00 (d, 1H, J=7.7 Hz),4.12-4.05 (m, 2H), 3.65-3.49 (m, 3H), 3.39 (s, 3H), 2.04-1.97 (m, 2H),1.80-1.73 (m, 2H); IR (neat) 2934, 2219, 1591, 1498, 1458, 1325, 1187,1146 cm⁻¹

A-46:4-butoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (CDCl₃) δ 7.89 (dd, 1H, J=7.7, 0.7 Hz), 6.99 (d, 1H, J=7.7 Hz),4.13-4.05 (m, 2H), 3.64-3.55 (m, 3H), 3.48 (t, 2H, J=6.4 Hz), 2.02-1.93(m, 2H), 1.79-1.68 (m, 2H), 1.62-1.53 (m, 2H), 1.45-1.33 (m, 2H), 0.93(t, 3H, J=7.5 Hz); IR (neat) 2956, 2219, 1592, 1499, 1458, 1324, 1187,1147, 959 cm⁻¹

A-47:4-isopropoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (CDCl₃) δ 7.89 (dd, 1H, J=7.7, 0.7 Hz), 6.99 (d, 1H, J=7.9 Hz),4.18-4.10 (m, 2H), 3.81-3.64 (m, 2H), 3.60-3.52 (m, 2H), 2.00-1.91 (m,2H), 1.76-1.65 (m, 2H), 1.18 (d, 6H, J=6.1 Hz); IR (neat) 2971, 2220,1592, 1499, 1458, 1324, 1236, 1185, 1147, 1039 cm⁻¹

A-48:4-ethoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (CDCl₃) δ 7.89 (dd, 1H, J=7.9, 0.7 Hz), 6.99 (d, 1H, J=7.7 Hz),4.18-4.10 (m, 2H), 3.64-3.51 (m, 5H), 2.04-1.95 (m, 2H), 1.79-1.68 (m,2H), 1.23 (t, 3H, J=7.1 Hz); IR (neat) 2931, 2219, 1592, 1497, 1458,1326, 1186, 1146, 1078 cm⁻¹

A-49:4-methylene-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (CDCl₃) δ 7.91 (d, 1H, J=7.9 Hz), 7.01 (d, 1H, J=7.9 Hz), 4.83(s, 2H), 3.85 (t, 4H, J=5.7 Hz), 2.39 (t, 4H, J=5.9 Hz); IR (neat) 2946,2220, 1591, 1495, 1458, 1333, 1238, 1191, 1147, 1088 cm⁻¹

A-50: 2-(6-aza-spiro[2.5]oct-6-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 7.88 (d, 1H, J=7.7 Hz), 6.97 (d, 1H, J=7.7 Hz), 3.87(m, 4H), 1.53 (m, 4H), 0.40 (s, 4H); IR (neat) 2925, 2219, 1591, 1496,1457, 1332, 1237, 1189, 1147, 960 cm⁻¹

A-51:3-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (CDCl₃) δ 7.87 (d, 1H, J=7.7 Hz), 6.95 (d, 1H, J=7.9 Hz),4.47-4.36 (m, 2H), 3.09-3.00 (m, 1H), 2.79-2.71 (m, 1H), 1.92-1.60 (m,4H), 1.27-1.14 (m, 1H), 0.97 (d, 3H, J=6.6 Hz); IR (neat) 2930, 2219,1592, 1565, 1499, 1457, 1320, 1240, 1187, 1147 cm⁻¹

A-52:2-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (CDCl₃) δ 7.87 (d, 1H, J=7.7 Hz), 6.93 (d, 1H, J=7.9 Hz), 4.85(m, 1H), 4.34 (m, 1H), 3.23 (m, 1H), 1.80-1.55 (m, 6H), 1.33 (d, 3H,J=6.8 Hz);

IR (neat) 2941, 2218, 1592, 1485, 1343, 1189, 1147, 1074 cm⁻¹

A-53:4-[(3-cyano-6-trifluoromethyl-pyridin-2-ylamino)-methyl]-piperidine-1-carbonicacid tert-butyl ester

¹H NMR (CDCl₃) δ 7.80 (d, 1H, J=7.7 Hz), 6.95 (d, 1H, J=7.7 Hz), 5.45(m, 1H), 4.11 (m, 2H), 3.48 (m, 2H), 2.70 (m, 2H), 1.80-1.65 (m, 3H),1.46 (s, 9H), 1.25-1.13 (m, 2H); IR (neat) 3369, 2926, 2223, 1685, 1599,1533, 1424, 1281, 1178, 1146 cm⁻¹

A-54:4-oxo-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (CDCl₃) δ 8.00 (d, 1H, J=7.9 Hz), 7.15 d, 1H, J=7.9 Hz), 4.13 (t,4H, J=6.0 Hz), 2.66 (t, 4H, J=6.2 Hz); IR (neat) 2976, 2221, 1713, 1567,1460, 1338, 1236, 1187, 1143, 1099 cm⁻¹

A-55:6″-trifluoromethyl-3,4,5,6,3′,4′,5′,6′-octahydro-2H,2′H-[1,4′;1′,2″]terpyridine-3″-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.88 (d, 1H, J=7.7 Hz), 6.98 (d, 1H, J=7.89Hz), 4.61 (d, 2H, J=13 Hz), 3.08 (dd, 2H, J=13.4, 13.4 Hz), 2.58-2.51(m, 5H, J=4.8 Hz), 1.97 (d, 2H, J=12.1 Hz), 1.72-1.56 (m, 6H), 1.45 (d,2H, J=5.3 Hz); IR (neat) 2854, 2218, 1336, 1240, 958, 822 cm⁻¹; MS (FAB)m/z 339 (M+H)

A-56:4-pyrrolidin-1-yl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.88 (d, 1H, J=7.9 Hz), 6.98 (d, 1H, J=7.9 Hz), 4.51 (d, 2H, J=13.0 Hz),3.23-3.13 (m, 2H), 2.60 (s, 4H), 2.33-2.25 (m, 1H), 2.05-2.01 (m, 2H),1.83-1.78 (m, 4H), 1.71-1.59 (m, 2H); IR(neat) 2959, 2219, 1238, 1083,960, 824, 743 cm⁻¹; MS (FAB) m/z 325(M+H)

A-57:4-morpholin-4-yl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.91 (d, 1H, J=7.9 Hz), 7.01 (d, 1H, J=7.7 Hz), 4.58 (d, 2H, J=13.2 Hz),3.75-3.70 (m, 5H), 3.15-3.06 (m, 2H), 2.61-2.45 (m, 4H), 2.01 (d, 2H,J=11.5 Hz), 1.69-1.56 (m, 2H); IR (neat) 2956, 2855, 2218, 1236, 1027,958, 876 cm⁻¹; MS (FAB) m/z 341(M+H)

A-58:4-ethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (400 MHz, CDCl₃)

7.85 (d, 1H, J=7.6 Hz), 6.93 (d, 1H, J=7.6 Hz), 4.53 (d, 2H, J=13.2 Hz),3.02 (dd, 2H, J=13.2, 13.2 Hz), 1.82 (d, 2H, J=12.4 Hz), 1.45-1.42 (m,1H), 1.33-1.28 (m, 4H), 0.90 (t, 3H, J=7.2 Hz); IR(neat)) 2854, 2218,1008, 911, 841, 744 cm⁻¹; MS (FAB) m/z 284(M+H)

A-59:4-benzyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.87 (d, 1H, J=7.9 Hz), 7.35-7.22 (m, 5H), 6.96 (d, 1H, J=7.7 Hz), 4.54(m, 2H), 3.00 (td, 2H, J=6.7, 2.4 Hz), 2.59 (d, 2H, J=6.8 Hz), 1.88-1.83(m, 3H), 1.39 (m, 2H); IR (neat) 2921, 2230, 1590, 1498, 1455, 1320,1240, 1145, 958, 745, 701 cm⁻¹; MS (FAB) m/z 346 (M+H)

A-60: 2-(3,4-dimethyl-phenylamino)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃),

7.92 (d, 1H, J=7.9 Hz), 7.43 (dd, 1H, J=8.1, 2.3 Hz), 7.38 (d, 1H, J=2.2Hz), 7.14 (d, 1H, J=8.1 Hz), 7.10 (d, 1H, J=7.7 Hz), 2.28 (s, 3H), 2.26(s, 3H); IR (neat) 3315, 2922, 2228, 1595, 1532, 1453, 1428, 1350, 1271,1199, 1141, 968, 820 cm⁻¹; MS (FAB) m/z 292 (M+H)

A-61:2-(5-chloro-2-methyl-phenylamino)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.12 (d, 1H, J=2.2 Hz), 7.98 (d, 1H, J=7.9Hz), 7.18 (d, 2H, J=7.9H), 7.10 (dd, 1H, J=8.1, 2.2 Hz), 2.32 (s, 3H);IR (neat) 3424, 2231, 1589, 1536, 1452, 1349, 1273, 1189, 1136, 960,899, 837, 802 cm⁻¹; MS (FAB) m/z 312 (M+H)

A-62: 2-(4-chloro-benzylamino)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.88 (d, 1H, J=7.7 Hz), 7.33 (s, 4H), 6.99 (d, 1H, J=7.8 Hz), 5.72 (bs,1H), 4.69 (d, 2H, J=5.7 Hz); IR (neat) 3372, 2221, 1598, 1531, 1404,1349, 1278, 1136, 907, 823, 793 cm⁻¹; MS (FAB) m/z 312 (M+H)

A-63: 2-(4-fluoro-phenylamino)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.96 (d, 1H, J=7.9 Hz), 7.65-7.57 (m, 2H),7.16-7.08 (m, 3H); IR (neat) 3362, 2226, 1619, 1592, 1546, 1508, 1463,1435, 1350, 1271, 1194, 1142, 961, 831 cm⁻¹; MS (FAB) m/z 282 (M+H)

A-64: 2-(4-chloro-phenylamino)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CD₃OD)

7.98 (d, 1H, J=7.9 Hz), 7.61 (d, 2H, J=9.0 Hz), 7.35 (d, 2H, J=8.8 Hz),7.18 (d, 1H, J=7.9 Hz); IR (neat) 2230, 1614, 1538, 1490, 1435, 1312,1262, 1173, 1138, 827, 696 cm⁻¹; MS (FAB) m/z 298 (M+H)

A-65: 2-phenylamino-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CD₃OD)

7.96 (d, 1H, J=7.7 Hz), 7.66 (d, 2H, J=8.8 Hz), 7.40 (t, 2H, J=7.5 Hz),7.16 (m, 2H); IR (neat) 3341, 2230, 1611, 1539, 1496, 1446, 1413, 1350,1271, 1195, 1139, 959, 828, 752, 691 cm⁻¹; MS (FAB) m/z 264 (M+H)

A-66: 2-azepan-1-yl-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃)

7.56 (d, 1H, J=8.1 Hz), 7.03 (s, 1H), 6.90 (d, 1H, J=8.1 Hz), 3.74-3.63(m, 4H), 1.98-1.83 (m, 4H), 1.69-1.51 (m, 4H); IR (neat) 2931, 2213,1616, 1560, 1503, 1444, 1316, 1171, 1131, 1081, 1001, 939, 859, 810cm⁻¹; MS (FAB) m/z 269 (M+H)

A-67:2-(4-pyridin-4-yl-piperazin-1-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.33 (d, 2H, J=6.4 Hz), 7.98 (d, 1H, J=7.9 Hz), 7.12 (d, 1H, J=7.9 Hz),6.69 (d, 2H, J=6.6 Hz), 4.08-4.36 (m, 4H), 3.58-3.45 (m, 4H); IR (neat)2917, 2230, 1592, 1481, 1445, 1390, 1321, 1236, 1139, 867, 804, 740cm⁻¹; MS (FAB) m/z 334 (M+H)

A-68:2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.85 (d, 1H, J=7.7 Hz), 7.08 (d, 1H, J=7.7Hz), 7.12-6.93 (m, 4H), 4.14-4.00 (m, 4H), 3.32-3.21 (m, 4H); IR (neat)2828, 2219, 1590, 1509, 1449, 1319, 1234, 1185, 1147, 1086, 970, 824,743, 704 cm⁻¹; MS (FAB) m/z 351 (M+H)

A-69:2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.95 (d, 1H, J=7.9 Hz), 7.07 (d, 1H, J=7.9Hz), 7.06-6.96 (m, 4H), 4.12-4.01 (m, 4H), 3.34-3.22 (m, 4H); IR (neat)2851, 2219, 1590, 1501, 1448, 1380, 1344, 1319, 1238, 1185, 1146, 1086,970, 820, 754 cm⁻¹; MS (FAB) m/z 351 (M+H)

A-70: 2-(4-phenyl-piperazin-1-yl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.94 (d, 1H, J=7.7 Hz), 7.35-7.28 (m, 2H), 7.06 (d, 1H, J=7.9 Hz),6.99-6.87 (m, 3H), 4.06-3.98 (m, 4H), 3.42-3.37 (m, 4H); IR (neat) 2850,2219, 1591, 1496, 1448, 132, 1233, 1185, 1146, 1086, 970, 825, 759, 694cm⁻¹; MS (FAB) m/z 333 (M+H)

A-71: 2-(methyl-phenyl-amino)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.79 (d, 1H, J=7.7 Hz), 7.47 (m, 2H), 7.29 (m,2H), 7.03 (d, 1H, J=7.8 Hz), 6.78 (m, 1H), 3.54 (s, 3H); IR (neat) 2920,2230, 1587, 1495, 1402, 1345, 1315, 1251, 1193, 1145, 942, 826, 745, 698cm⁻¹; MS (FAB) m/z 278 (M+H)

A-72:4,4-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.87 (d, 1H, J=7.9 Hz), 6.96 (d, 1H, J=7.9 Hz), 3.87-3.73 (m, 4H),1.61-1.46 (m, 4H), 1.03 (s, 6H); IR (neat) 2924, 2218, 1591, 1566, 1498,1463, 1346, 1320, 1241, 1182, 1147, 1082, 956, 823, 744 cm⁻¹; MS (FAB)m/z 284 (M+H)

A-73: 2-(4-p-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃)

7.71 (d, 1H, J=8.1 Hz), 7.26 (d, 1H, J=7.9 Hz), 7.25 (s, 1H), 7.11 (d,2H, J=8.4 Hz), 6.91 (d, 2H, J=8.6 Hz), 3.52-3.41 (m, 4H), 3.43-3.37 (m,4H), 2.29 (s, 3H); IR (neat) 2838, 2227, 1615, 1517, 1432, 1308, 1240,1178, 1121, 1079, 963, 809 cm⁻¹; MS (FAB) m/z 346 (M+H)

A-74: 2-(4-m-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃)

7.71 (d, 1H, J=8.4 Hz), 7.26 (d, 1H, J=7.7 Hz), 7.24 (s, 1H), 7.19 (t,1H, J=7.9 Hz), 6.81 (s, 1H), 6.80 (d, 1H, J=7.1 Hz), 6.74 (d, 1H, J=7.7Hz), 3.49-3.31 (m, 8H), 2.34 (s, 3H); IR (neat) 2837, 2231, 1605, 1497,1432, 1311, 1252, 1174, 1133, 1078, 964, 829, 777 cm⁻¹; MS (FAB) m/z 346(M+H)

A-75:4-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.72 (d, 1H, J=7.9 Hz), 7.53 (d, 2H, J=8.8Hz), 7.29 (d, 1H, J=8.0 Hz), 7.25 (s, 1H), 6.99 (d, 2H, J=8.6 Hz),3.57-3.41 (m, 8H); IR (neat) 2842, 2225, 1615, 1527, 1501, 1432, 1388,1332, 1235, 1116, 1073, 962, 827, 735 cm⁻¹; MS (FAB) m/z 400 (M+H)

A-76:2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.63 (d, 1H, J=7.9 Hz), 7.19 (d, 1H, J=7.6Hz), 7.18 (s, 1H), 6.93-6.82 (m, 4H), 3.72 (s, 3H), 3.43-3.35 (m, 4H),3.28-3.21 (m, 4H); IR (neat) 2962, 2837, 2228, 1515, 1432, 1306, 1261,1176, 1117, 1036, 962, 821 cm⁻¹; MS (FAB) m/z 362 (M+H)

A-77:2-[4-(4-fluoro-phenyl)-3,6-dihydro-2H-pyridin-1-yl]-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃)

7.68 (d, 1H, J=8.0 Hz), 7.40 (m, 2H), 7.22 (s, 1H), 7.18 (d, 1H, J=8.0Hz), 7.05 (m, 2H), 6.11 (m, 1H), 3.98 (bq, 2H, J=3.1 Hz), 3.71 (t, 2H,J=5.5 Hz), 2.79 (m, 2H); IR (neat) 2919, 1683, 1601, 1509, 1440, 1332,1229, 1173, 1134, 838 cm⁻¹; MS (FAB) m/z 347 (M+H)

A-78: 2-(butyl-methyl-amino)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=7.9 Hz), 6.89 (d, 1H, J=7.7 Hz), 3.72 (t, 2H, J=7.7 Hz),3.33 (s, 3H), 1.60-1.75 (m, 2H), 1.30-1.46 (m, 2H), 0.96 (t, 3H, J=7.4Hz); IR (neat) 2962, 2230, 1594, 1517, 1417, 1328, 1239, 1186, 1147, 818cm⁻¹; MS (FAB) m/z 258 (M+H)

A-79: 2-(4-phenyl-piperazin-1-yl)-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.70 (d, 1H, J=8.2 Hz), 7.23-7.33 (m, 4H),6.87-7.02 (m, 3H), 3.35-3.50 (m, 8H); IR (KBr) 2834, 2224, 1600, 1499,1432, 1311, 1229, 1174, 1132, 1078, 962, 878, 828, 760 cm⁻¹; MS (FAB)m/z 332 (M+H)

A-80: 2-azocan-1-yl-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃)

7.56 (d, 1H, J=8.1 Hz), 7.00 (s, 1H), 6.86 (dd, 1H, J=8.2, 1.3 Hz),3.71-3.79 (m, 4H), 1.79-1.91 (m, 4H), 1.50-1.69 (m, 6H);

IR (neat) 2926, 2223, 2210, 1617, 1558, 1505, 1446, 1317, 1171, 1131,1078, 989, 808 cm⁻¹; MS (FAB) m/z 283 (M+H)

A-81: 2-(4,4-dimethyl-piperidin-1-yl)-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.64 (d, 1H, J=7.9 Hz), 7.21 (s, 1H), 7.16 (d,1H, J=7.9 Hz), 3.22-3.29 (m, 4H), 1.55-1.64 (m, 4H), 1.03 (s, 6H); IR(neat) 2954, 2223, 1612, 1567, 1500, 1431, 1347, 1311, 1239, 1173, 1134,1078, 952, 874, 825 cm⁻¹; MS (FAB) m/z 283 (M+H)

A-82: 244-ethyl-piperidin-1-yl)-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃)

7.64 (d, 1H, J=7.9 Hz), 7.13-7.21 (m, 2H), 3.62-3.73 (m, 2H), 2.79-2.92(m, 2H), 1.81-1.90 (m, 2H), 1.25-1.55 (m, 5H), 0.94 (t, 3H, J=7.0 Hz);IR (neat) 2930, 2224, 1612, 1567, 1500, 1433, 1312, 1247, 1216, 1174,1133, 1078, 953, 877, 825 cm⁻¹; MS (FAB) m/z 283 (M+H)

A-83: 2-dipropylamino-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.58 (d, 1H, J=8.0 Hz), 7.04 (s, 1H), 6.97 (d,1H, J=8.0 Hz), 3.35-3.42 (m, 4H), 1.58-1.72 (m, 4H), 0.89-0.97 (m, 6H)

IR (neat) 2966, 2223, 1616, 1561, 1505, 1447, 1320, 1230, 1173, 1133,1078, 992, 813 cm⁻¹; MS (FAB) m/z 271 (M+H)

A-84:4-trifluoromethyl-2-(4-trifluoromethyl-piperidin-1-yl)-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.69 (d, 1H, J=8.0 Hz), 7.18-7.29 (m, 2H),3.69-3.79 (m, 2H), 2.83-2.93 (m, 2H), 2.22 (m, 1H), 1.99-2.10 (m, 2H),1.81-1.99 (m, 2H); IR (neat) 2963, 2230, 1613, 1500, 1435, 1391, 1336,1311, 1256, 1139, 1080, 955, 900, 830 cm⁻¹; MS (FAB) m/z 323 (M+H)

A-85: 2-(4-benzyl-piperidin-1-yl)-4-trifluoromethyl-benzonitrile

¹H NMR (400 MHz, CDCl₃) δ 7.80 (dd, 1H, J=7.6, 7.6 Hz), 7.64 (d, 1H,J=8.4 Hz), 7.56 (d, 1H, J=8.4 Hz), 7.52 (d, 1H, J=8.4 Hz), 7.27-7.32 (m,2H), 7.15-7.24 (m, 2H), 3.61-3.66 (m, 2H), 2.77-2.86 (m, 2H), 2.62 (d,2H, J=7.2 Hz), 1.78-1.85 (m, 2H), 1.72 (m, 1H), 1.49-1.60 (m, 2H); IR(neat) 2922, 2230, 1612, 1499, 1434, 1312, 1174, 1133, 1077, 953, 827,746, 701 cm⁻¹; MS (FAB) m/z 345 (M+H)

A-86:4-acetyl-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.90 (d, 1H, J=7.7 Hz), 7.25-7.44 (m, 5H),7.01 (d, 1H, J=7.9 Hz), 4.10-4.25 (m, 2H), 3.51-3.63 (m, 2H), 2.50-2.62(m, 2H), 2.13-2.27 (m, 2H), 1.97 (s, 3H); IR (neat) 2924, 2223, 1704,1590, 1494, 1455, 1350, 1320, 1243, 1138, 959, 912, 743, 701 cm⁻¹; MS(FAB) m/z 374 (M+H)

A-87:6-(chloro-difluoro-methyl)-2-(4-phenyl-piperazin-1-yl)-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.94 (d, 1H, J=7.9 Hz), 7.24-7.34 (m, 2H),7.04 (d, 1H, J=7.9 Hz), 6.87-7.00 (m, 3H), 4.00-4.06 (m, 4H), 3.32-3.39(m, 4H); IR (neat) 2916, 2230, 2217, 1590, 1497, 1449, 1341, 1230, 1081,986, 934, 812, 761, 693 cm⁻¹; MS (FAB) m/z 349 (M+H)

A-88: 2-dipropylamino-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.74 (dd, 1H, J=7.8, 0.7 Hz), 6.75 (d, 1H, J=7.7 Hz), 3.53 (tt, 4H,J=7.7, 1.8 Hz), 1.70-1.66 (m, 4H), 0.86 (t, 4H, J=7.3 Hz); IR (neat)2969, 2215, 1594, 1565, 1512, 1459, 1331 cm⁻¹; MS (FAB) m/z 272 (M+H)

A-89:6′-tert-butyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.65 (d, 1H, J=7.9 Hz), 6.70 (d, 1H, J=7.9 Hz), 3.70-3.68 (bs, 4H), 1.65(s, 6H), 1.30 (s, 9H); IR (neat) 2934, 2856, 2213, 1583, 1550, 1447,1362 cm⁻¹; MS (FAB) m/z 244 (M+H)

A-90: 6-tert-butyl-2-pyrrolidin-1-yl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.61 (d, 1H, J=8.1 Hz), 6.59 (d, 1H, J=8.1 Hz), 3.80 (m, 4H), 2.00 (m,4H), 1.28 (s, 9H); IR (neat) 3409, 2964, 2785, 2210, 1583, 1552, 1456cm⁻¹; MS (FAB) m/z 230 (M+H)

A-91:6′-tert-butyl-4-methyl-3,4,5,6-tetrahydro-2H[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.57 (d, 1H, J=7.9 Hz), 6.63 (d, 1H, J=8 Hz), 4.37 (m, 2H), 2.90 (td,2H, J=12.6, 2.4 Hz), 1.68-1.16 (m, 5H), 1.22 (s, 9H), 0.83 (d, 3H, J=7.5Hz); IR (neat) 2956, 2869, 2213, 1582, 1550, 1452, 1367 cm⁻¹; MS (FAB)m/z 258 (M+H)

A-92: 6-tert-butyl-2-dipropylamino-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.61 (d, 1H, J=8.0 Hz), 6.59 (d, 1H, J=8.0 Hz), 3.58 (t, 4H, J=7.9 Hz),1.68-1.64 (m, 4H), 1.28 (s, 9H), 0.95 (t, 6H, J=7.3 Hz); IR (neat) 2964,2873, 2208, 1585, 1550, 1495, 1456 cm⁻¹; MS (FAB) m/z 320 (M+H)

A-93: 2-azepan-1-yl-6-tert-butyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.60 (d, 1H, J=8.0 Hz), 6.60 (d, 1H, J=8.0 Hz), 3.90 (t, 4H, J=5.9 Hz),1.89-1.85 (m, 4H), 1.59-1.43 (m, 4H), 1.28 (s, 9H); IR (neat) 2930,2859, 2208, 1584, 1549, 1487, 1453 cm⁻¹; MS (FAB) m/z 258 (M+H)

A-94:6′-tert-butyl-4-phenyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.69 (d, 1H, J=8.0 Hz), 7.38-7.19 (m, 5H), 6.76 (d, 1H, J=7.7 Hz), 4.60(d, 2H, J=6.2 Hz), 3.10 (td, 2H, J=12.5, 2.8 Hz), 2.79 (m, 1H),2.00-1.78 (m, 4H), 1.3 (s, 9H); IR (neat) 2959, 2213, 1583, 1550, 1452,1368 1223 cm⁻¹, MS (FAB) m/z 320 (M+H)

A-95:4-hydroxymethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.89 (d, 1H, J=7.9 Hz), 6.99 (d, 1H, J=7.9Hz), 4.58 (d, 1H, J=13.6 Hz), 3.57 (t, 2H, J=5.9 Hz), 3.01 (m, 2H),1.92-1.87 (m, 3H), 1.41-1.34 (m, 2H); IR (neat) 2923, 2220, 1591, 1567,1499, 1458, 1364 cm⁻¹; MS (FAB) m/z 286 (M+H)

A-96:6-tert-butyl-2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.70 (d, 1H, J=8.0 Hz), 7.02-6.89 (m, 4H), 6.81 (d, 1H, J=8.0 Hz),3.92-3.88 (m, 4H), 3.26-3.23 (m, 4H), 1.30 (s, 9H); IR (neat) 2963,2215, 1584, 1550, 1511, 1445, 1363 cm⁻¹; MS (FAB) m/z 339 (M+H)

A-97: 2-diethylamino-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=7.9 Hz), 7.07 (d, 1H, J=7.7 Hz), 3.74 (q, 4H, J=7.0 Hz),1.30 (t, 6H, J=7.1 Hz); IR (KBr) 2983, 2216, 1594, 1566, 1514, 1459,1330 cm⁻¹; MS (FAB) m/z 243 (M+H)

A-98: 2-dimethylamino-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.87 (d, 1H, J=7.9 Hz), 6.92 (d, 1H, J=7.7 Hz), 3.35 (s, 4H); IR (KBr)2940, 2218, 1595, 1525, 1411, 1320, 1265 cm⁻¹ MS (FAB) m/z 215 (M+H)

A-99: 2-dibutylamino-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.84 (d, 1H, J=7.7 Hz), 6.85 (d, 1H, J=7.9 Hz), 3.66 (t, 4H, J=7.9 Hz),1.72-1.60 (m, 4H), 1.45-1.32 (m, 4H), 0.97 (t, 6H, J=7.3 Hz); IR (KBr)2962, 271, 2215, 1594, 1566, 1513, 1461 cm⁻¹; MS (FAB) m/z 300 (M+H)

A-100: 2-benzylamino-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.87 (d, 1H, J=7.7 Hz), 7.40-7.26 (m, 5H),6.97 (d, 1H, J=7.7 Hz); IR (KBr) 3357, 2228, 1560, 1534, 1424, 1343,1282 cm⁻¹; MS (FAB) m/z 277 (M+H)

A-101:4-benzyl-4′-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.14-7.34 (m, 5H), 6.90 (bs, 1H), 4.39-4.49(m, 2H), 2.90-3.02 (m, 2H), 2.59 (d, 2H, J=6.8 Hz), 2.52 (bs, 3H),1.71-1.87 (m, 2H), 1.22-1.50 (m, 3H); IR (neat) 2922, 2850, 2214, 1577,1494, 1452, 1391, 1243, 1182, 1143, 967, 913, 743, 701 cm⁻¹; MS (FAB)m/z 360 (M+H)

A-102:4,4′-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 6.89 (s, 1H), 4.42 (m, 2H), 3.02 (m, 2H), 2.52(s, 3H), 1.65-1.79 (m, 3H), 1.33 (m, 2H), 0.99 (d, 3H, J=6.3 Hz); IR(neat) 2923, 2215, 1577, 1453, 1391, 1315, 1241, 1182, 1145, 1078, 969,913, 847, 740 cm⁻¹; MS (FAB) m/z 284 (M+H)

Stage 2: Method 1:

Compounds of the general formula VI-B (5 mmol), in which R⁵, R¹², R¹³,U, T and V have the above-stated meaning and m denotes 0, 1, 2 or 3,palladium on carbon (10%, 500 mg) and concentrated hydrochloric acid (3mL) are dissolved in MeOH (30 mL) and exposed to a hydrogen atmospherefor 6 hours at RT. The reaction mixture is filtered through celite andthe filtrate is evaporated under a vacuum. The residue is purified bymeans of flash chromatography (SiO₂, EA).

The following compounds B-1 to B-15 were obtained according to theabove-stated general method:

Compound B-1[2-(piperidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl]methylamine

The compound was obtained in a yield of 50% as a pale yellow oil.

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=5.7 Hz), 7.26 (d, 1H, J=5.7 Hz), 4.01 (s, 2H), 3.11 (bs,4H), 1.62-1.70 (m, 6H)

Compound B-2[2-(morpholin-4-yl)-6-(trifluoromethyl)-pyridin-3-yl]methylamine

The compound was obtained in a yield of 28% as a pale yellow oil.

¹H NMR (400 MHz, CDCl₃)

7.86 (d, 1H, J=5.7 Hz), 7.31 (d, 1H, J=5.7 Hz), 3.93 (s, 2H), 3.85 (t,4H, J=3.3 Hz), 3.23 (t, 4H, J=3.3 Hz)

Compound B-3[2-(pyrrolidin-1-yl)-6-(trifluoromethyl)-pyridin-3-yl]methylamine

The compound was obtained in a yield of 60% as a pale yellow oil.

¹H NMR (300 MHz, CDCl₃) δ 7.58 (d, 1H, J=7.5 Hz), 6.98 (d, 1H, J=7.5Hz), 3.93 (s, 2H), 3.55-3.60 (m, 4H), 1.93-1.97 (m, 4H)

Compound B-4 2-(piperidin-1-yl)-4-(trifluoromethyl)benzylamine

The compound was obtained in a yield of 50% as a pale yellow oil.

¹H NMR (300 MHz, CD₃OD) δ 7.59 (d, 1H, J=7.8 Hz), 7.52 (s, 1H), 7.47 (d,1H, J=7.8 Hz), 4.28 (s, 2H), 2.89-2.93 (m, 4H), 1.63-1.82 (m, 6H)

Compound B-5 2-(morpholin-4-yl)-4-(trifluoromethyl)benzylamine

The compound was obtained in a yield of 38% as a pale yellow oil.

¹H NMR (300 MHz, CD₃OD) δ 7.61 (d, 1H, J=7.8 Hz), 7.55 (s, 1H), 7.50 (d,1H, J=7.8 Hz), 4.26 (s, 2H), 3.87 (t, 4H, J=4.5 Hz), 2.95 (t, 4H, J=4.5Hz)

Compound B-6 2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzylamine

The compound was obtained in a yield of 55% as a pale yellow oil.

¹H NMR (300 MHz, CD₃OD) δ 7.88 (d, 1H, J=7.8 Hz), 7.25 (s, 1H), 7.18 (d,1H, J=7.8 Hz), 4.21 (s, 2H), 3.15-3.19 (m, 4H), 1.95-1.99 (m, 4H)

B-7:C-[4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.03 (d, 1H, J=7.5 Hz), 7.41 (d, 1H, J=7.5 Hz), 7.24 (m, 2H), 7.01 (dd,1H, J=8.1, 8.4 Hz), 4.26 (s, 2H), 3.45 (m, 2H), 3.07 (m, 2H), 2.72 (m,1H), 1.89-1.96 (m, 4H); IR (neat) 2913, 2846, 1593, 1512, 1469, 1422,1368, 1225, 1190, 1152, 950, 839 cm⁻¹; MS (FAB) m/z 354(M+H)

B-8:4-(2,2-dimethyl-propionyloxy)-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.81 (d, 1H, J=7.7 Hz), 7.31 (d, 1H, J=7.7 Hz), 4.98(m, 1H), 4.35 (s, NH3+), 3.97 (s, 2H), 3.40-3.31 (m, 2H), 3.18-3.10 (m,2H), 2.06-1.98 (m, 2H), 2.04 (s, 3H), 1.87-1.77 (m, 2H), 1.22 (s, 9H);IR (neat) 2970, 1724, 1593, 1462, 1419, 1168, 1033 cm⁻¹

B-9:4-acetoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.81 (d, 1H, 7.7 Hz), 7.31 (d, 1H, 7.7 Hz), 4.97 (m,1H), 4.03-3.93 (m, 5H), 3.45-3.35 (m, 2H), 3.14-3.05 (m, 1H), 2.08 (s,3H), 2.10-1.98 (m, 2H), 1.88-1.77 (m, 2H); IR (neat) 2957, 1734, 1419,1247, 1138, 1034 cm⁻¹

B-10:4-methoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.80 (d, 1H, J=7.5 Hz), 7.29 (d, 1H, J=7.7 Hz), 4.28(bs, NH3), 3.97 (s, 2H), 3.47-3.36 (m, 6H), 3.02-2.94 (m, 2H), 2.09-2.01(m, 5H), 1.77-1.65 (m, 2H); IR (neat) 2930, 1542, 1461, 1418, 1335,1178, 1137, 957 cm⁻¹

B-11:4-butoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.80 (d, 1H, J=7.7 Hz), 7.29 (d, 1H, J=7.7 Hz),4.03-3.98 (m, 5H, 2H+NH3), 3.49 (t, 2H, J=6.6 Hz), 3.47-3.37 (m, 3H),3.01-2.93 (m, 2H), 2.07-1.97 (m, 2H), 1.98 (s, 3H), 1.77-1.65 (m, 2H),1.62-1.55 (m, 2H), 1.45-1.33 (m, 2H), 0.92 (t, 3H, J=7.3 Hz); IR (neat)2955, 1542, 1462, 1419, 1333, 1140, 1041 cm⁻¹

B-12:4-ethoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.80 (d, 1H, J=7.7 Hz), 7.29 (d, 1H, J=7.7 Hz), 5.30(bs, NH3), 3.59-3.39 (m, 5H), 3.01-2.93 (m, 2H), 2.08-2.00 (m, 5H),1.78-1.66 (m, 2H), 1.23 (t, 3H, J=7.0 Hz); IR (neat) 2927, 1593, 1419,1333, 1241, 1178, 1139 cm⁻¹

B-13:C-(5′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,3′]bipyridinyl-2′-yl)-methylamine

¹H NMR (300 MHz, D₂O) δ 8.71 (s, 1H), 8.21 (s, 1H), 4.45 (s, 2H), 3.24(d, 4H, J=4.6 Hz), 1.77 (s, 4H), 1.51 (s, 2H); MS (FAB) m/z 260 (M+H)

B-14: 2-(4-ethyl-piperidin-1-yl)-4-trifluoromethyl-benzylamine

¹H NMR (400 MHz, CDCl₃) δ 7.43 (d, 1H, J=6.0 Hz), 7.27-7.33 (m, 2H),3.92 (s, 2H), 3.04-3.12 (m, 2H), 2.63-2.72 (m, 2H), 1.78-1.85 (m, 2H),1.24-1.43 (m, 5H), 0.93 (bt, 3H); IR (neat) 2925, 1423, 1337, 1311,1242, 1165, 1123, 1080, 949, 826 cm⁻¹; MS (FAB) m/z 287 (M+H)

B-15:4-isopropoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.78 (d, 1H, J=7.7 Hz), 7.28 (d, 1H), 4.26 (bs, NH3),3.95 (s, 2H), 3.76 (m, 1H), 3.57-3.40 (m, 3H), 2.97 (m, 2H), 2.07 (s,3H, AcO), 2.04-1.96 (m, 2H), 1.76-1.65 (m, 2H), 1.18 (d, 6H, J=6.2 Hz);IR (neat) 2972, 1593, 1462, 1419, 1333, 1177, 1140, 1041 cm⁻¹

Method 2:

Compounds of the general formula VI-B (2 mmol), in which R⁵, R¹², R¹³,U, T and V have the above-stated meaning and m denotes 0, 1, 2 or 3, aredissolved in THF (10 mL) and BH₃.S(CH₃)_(2 [)2.0 M in THF, 3 mL, 3equivalents] is added.

The reaction mixture is heated to reflux for 8 hours, aq. HCl (2 N) isadded and the reaction mixture is again heated to reflux for 30 minutes.Aq. NaOH soln. and EA are added. The combined organic extracts arewashed with sat. aq. NaCl soln. and dried over MgSO₄. The solvent isevaporated under a vacuum and the residue is purified by flashchromatography (SiO₂, different mixtures of methylene chloride andmethanol).

The following compounds B-16 to B-80 were obtained according to theabove-stated general method:

B-16:(6-(chlorodifluoromethyl)-2-(piperidin-1-yl)pyridin-3-yl)methanamine

¹H NMR (300 MHz, CDCl₃) δ 7.78 (d, 1H, J=7.8 Hz), 7.22 (d, 1H, J=7.8Hz), 3.90 (s, 2H), 3.12-3.16 (m, 4H), 1.60-1.70 (m, 6H)

IR (neat) 2935, 2851, 1590, 1417, 1373, 1300, 1091, 972, 913, 827 cm⁻¹MS (FAB) m/z 276 (M+H)

B-17:(2-(4-benzylpiperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methanamine

¹H NMR (300 MHz, CDCl₃) δ 7.81 (d, 1H, J=7.8 Hz), 7.23-7.37 (m, 6H),3.89 (s, 2H), 3.58 (s, 2H), 3.22-3.25 (m, 4H), 2.57-2.62 (m, 4H); IR(neat) 2814, 1592, 1417, 1324, 1176, 1135, 1005, 964, 836, 741, 700cm⁻¹; MS (FAB) m/z 351 (M+H)

B-18:(6-(trifluoromethyl)-2-(4-methylpiperidin-1-yl)pyridin-3-yl)methanamine

¹H NMR (300 MHz, CDCl₃) δ 7.89 (d, 1H, J=7.8 Hz), 7.33 (d, 1H, J=7.8Hz), 3.88 (s, 2H), 3.39 (m, 2H), 2.83 (m, 2H), 1.75 (m, 2H), 1.55 (m,1H), 1.38 (m, 2H), 1.00 (d, 3H, J=6.6 Hz); MS (FAB) m/z 274(M+H)

B-19:C-(4-fluoro-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.83 (d, 1H, J=7.8 Hz), 7.28 (d, 1H, J=7.8Hz), 4.85 (dm, 1H, J=48.3 Hz), 3.92 (s, 2H), 3.39 (m, 2H), 3.14 (m, 2H),2.01-2.28 (m, 4H); MS (FAB) m/z 278(M+H)

B-20;C-(6′-(chloro-difluoro-methyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yn-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.72 (d, 1H, J=7.5 Hz), 7.13 (d, 1H, J=7.5Hz), 3.84 (s, 2H), 3.37 (m, 2H), 2.77 (m, 2H), 1.68 (m, 2H), 1.48 (m,1H), 1.24 (m, 2H), 0.89 (d, 3H, J=6.6 Hz); IR (neat) 2923, 1590, 1452,1417, 1254, 1186 cm⁻¹; MS (FAB) m/z 290(M+H)

B-21:C-[2-azepan-1-yl-6-(chloro-difluoro-methyl)-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.69 (d, 1H, J=7.5 Hz), 6.97 (d, 1H, J=7.5Hz), 3.98 (s, 2H), 3.37 (m, 4H), 1.71 (m, 4H), 1.51 (m, 4H); IR (neat)3432, 2928, 2857, 1593, 1452, 1421, 1371, 1257 cm⁻¹; MS (FAB) m/z290(M+H)

B-22:C-[6′-(4-fluoro-phenyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) d 8.00 (m, 2H), 7.66 (d, 1H, J=7.8 Hz), 7.30 (d,1H, J=7.8 Hz), 7.10 (dd, 2H, J=8.7, 8.7 Hz), 3.90 (s, 2H), 3.43 (m, 2H),2.89 (m, 2H), 1.74 (m, 2H), 1.53 (m, 1H), 1.38 (m, 2H), 0.99 (d, 3H,J=6.3 Hz); IR (neat) 2932, 2851, 1600, 1577, 1509, 1447, 1421, 1372,1236, 1156, 1112, 1031 cm⁻¹; MS (FAB) m/z 300(M+H)

B-23: C[2-azepan-1-yl-6-(4-fluoro-phenyl)-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.97 (m, 2H), 7.59 (d, 1H, J=7.8 Hz), 7.17 (d,1H, J=7.8 Hz), 7.09 (dd, 2H, J=8.7, 8.7 Hz), 3.89 (s, 2H), 3.49 (t, 4H,J=6.0 Hz), 1.81 (m, 4H), 1.64 (m, 4H); IR (neat) 2925, 2853, 1576, 1508,1448, 1373, 1230, 1154, 906 cm⁻¹; MS (FAB) m/z 300(M+H)

B-24:[3-aminomethyl-6-(chloro-difluoro-methyl)-pyridin-2-yl]-dipropyl-amine

¹H NMR (300 MHz, CDCl₃) δ 7.68 (d, 1H, J=7.8 Hz), 7.06 (d, 1H, J=7.8Hz), 3.84 (s, 2H), 3.08 (t, 4H, J=7.5 Hz), 1.47 (m, 4H), 0.77 (t, 6H,J=7.2 Hz); IR (neat) 2964, 2874, 1591, 1462, 1418, 1372, 1257, 1091, 999cm⁻¹ MS (FAB) m/z 292(M+H)

B-25:C-[2-(1,3-dihydro-isoindol-2-yl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.63 (d, 1H, J=7.8 Hz), 7.27-7.31 (m, 4H),7.03 (d, 1H, J=7.8 Hz), 5.06 (s, 4H), 4.08 (s, 2H); IR (neat) 3365,2926, 2857, 1598, 1457, 1363, 1263, 1177, 1132, 1013, 820 cm⁻¹; MS (FAB)m/z 294(M+H)

B-26:3′-aminomethyl-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-carbonicacid ethyl ester

¹H NMR (300 MHz, CDCl₃) δ 7.83 (d, 1H, J=7.5 Hz), 7.45 (m, 2H), 7.35 (m,3H), 7.26 (d, 1H, J=8.1 Hz), 4.15 (q, 2H, J=7.2 Hz), 4.03 (s, 2H), 3.47(m, 2H), 3.08 (m, 2H), 2.69 (m, 2H), 2.10 (m, 2H), 1.21 (t, 3H, J=7.2Hz); MS (FAB) m/z 408 (M+H)

B-27:C-(4,6′-bis-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.80 (d, 1H, J=7.8 Hz), 7.23 (d, 1H, J=7.8Hz), 3.83 (s, 2H), 3.48 (m, 2H), 2.79 (m, 2H), 2.15 (m, 1H), 1.88 (m,2H), 1.65 (m, 2H); IR (neat) 2960, 1591, 121, 1378, 1337, 1255, 1141,1084, 955, 901, 837, 698 cm⁻¹; MS (FAB) m/z 328 (M+H)

B-28:C-(4-methoxymethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.81 (d, 1H, J=7.8 Hz), 7.26 (d, 1H, J=7.8 Hz), 3.91 (s, 2H), 3.36 (s,3H), 3.29 (d, 2H, J=6.0 Hz), 2.87 (m, 2H), 2.37 (s, 2H), 1.71-1.86 (m,4H), 1.34-1.47 (m, 3H); IR (neat) 2924, 1592, 1455, 1374, 1324, 1268,1175, 1135, 950, 835 cm⁻¹; MS (FAB) m/z 304(M+H)

B-29:C-[2-(4-p-tolyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.85 (d, 1H, J=7.8 Hz), 7.30 (d, 1H, J=7.8 Hz), 7.09 (d, 2H, J=8.4 Hz),6.88 (d, 2H, J=8.4 Hz), 3.94 (s, 2H), 3.37 (m, 4H), 3.26 (m, 4H), 2.27(s, 3H); IR (neat) 3368, 2847, 1732, 1591, 1515, 117, 1333, 1235, 1176,1137, 1051, 966, 916, 814, 755 cm⁻¹; MS (FAB) m/z 351(M+H)

B-30:C-[2-(4-m-tolyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=7.8 Hz), 7.31 (d, 1H, J=7.8 Hz), 7.18 (t, 1H, J=7.5 Hz),6.77-6.79 (m, 2H), 3.95 (s, 2H), 3.31-3.38 (m, 8H), 2.33 (s, 3H); IR(neat) 3367, 2845, 1595, 1493, 1418, 1335, 1240, 1335, 1137, 1045, 998,967, 836, 775, 695 cm⁻¹; MS (FAB) m/z 351 (M+H)

B-31:C-{2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-yl}-methylamine

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=7.8 Hz), 7.31 (d, 1H, J=7.8 Hz), 6.94 (d, 2H, J=6.9 Hz),(d, 2H, J=6.9 Hz), 3.95 (s, 2H), 3.77 (s, 3H), 3.39 (m, 4H), 3.22 (m,4H); IR (neat) 2837, 1590, 1512, 1418, 1332, 1244, 1178, 1137, 1035,967, 826 cm⁻¹; MS (FAB) m/z 367(M+H)

B-32:C-{6-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-pyridin-3-yl}-methylamine

¹H NMR (300 MHz, CDCl₃)

7.89 (d, 1H, J=7.8 Hz), 7.50 (d, 2H, J=7.8 Hz), 7.32 (d, 1H, J=7.8 Hz),6.97 (d, 2H, J=7.8 Hz), 4.09 (s, 2H), 3.40 (m, 8H), 2.27 (s, 2H); IR(neat) 2933, 1695, 1600, 1511, 1428, 1397, 1342, 1314, 1262, 1158, 1026,835 cm⁻¹; MS (FAB) m/z 405(M+H)

B-33:C-{6-trifluoromethyl-2-[4-(3-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-pyridin-3-yl}-methylamine

¹H NMR (300 MHz, CDCl₃) δ 8.46 (d, 1H, J=3.3 Hz), 7.86-7.93 (m, 2H),7.31 (d, 1H, J=7.5 Hz), 7.03 (m, 1H), 3.97 (s, 2H), 3.46 (m, 4H), 3.36(m, 4H), 2.12 (bs, 2H); IR (neat) 3367, 2850, 1590, 1445, 1368, 1312,1236, 1138, 1027, 966, 837 cm⁻¹; MS (FAB) m/z 407 (M+H)

B-34:C-[2-(4-cyclohexyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.80 (d, 1H, J=7.5 Hz), 7.27 (d, 1H, J=7.5 Hz), 3.90 (s, 2H), 3.25 (m,4H), 2.73 (m, 4H), 2.16 (m, 1H), 1.70 (m, 4H), 1.19-1.28 (m, 6H); MS(FAB) m/z 343(M+H)

B-35:2-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-ethylamine

¹H NMR (300 MHz, CDCl₃) δ 7.46 (d, 1H, J=7.5 Hz), 7.12 (d, 1H, J=7.5Hz), 3.32 (m, 2H), 2.95 (t, 2H, J=6.9 Hz), 2.75 (m, 4H), 1.55-1.63 (m,5H), 0.91 (d, 3H, J=6.3 Hz); IR (neat) 3364, 2924, 1648, 1590, 1457,1415, 1322, 1236, 1176, 1136, 1045, 944, 834 cm⁻¹; MS (FAB) m/z 288(M+H)

B-36:(3′-aminomethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]pyridinyl-4-yl)-phenyl-amine

¹H NMR (300 MHz, CDCl₃) δ 7.82 (d, 1H, J=7.5 Hz), 7.29 (d, 1H, J=7.5Hz), 7.18 (m, 2H), 6.66 (m, 3H), 3.93 (s, 2H), 3.47 (m, 2H), 3.03 (m,2H), 2.84 (bs, 2H), 2.18 (m, 2H), 1.58-1.66 (m, 3H); IR (neat) 3365,2938, 1598, 1504, 1421, 1333, 1265, 1177, 1136, 1044, 953, 836, 752, 695cm⁻¹; MS (FAB) m/z 351(M+H)

B-37:C-[2-(2,6-dimethyl-morpholin-4-yl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.77 (d, 1H, J=7.8 Hz), 7.20 (d, 1H, J=7.8 Hz), 3.84 (s, 2H), 3.73 (m,2H), 3.25 (m, 2H), 2.60 (m, 2H), 1.70 (bs, 2H), 1.15 (d, 6H, J=6.3 Hz);IR (neat) 2976, 1591, 1459, 1418, 1249, 1175, 1006, 836 cm⁻¹; MS (FAB)m/z 290 (M+H)

B-38:C-[2-(1,1-dioxo-thiomorpholin-4-yl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.94 (d, 1H, J=7.5 Hz), 7.38 (d, 1H, J=7.5 Hz), 3.82-3.91 (m, 6H), 3.20(m, 4H), 1.52 (bs, 2H); IR (neat) 2929, 1709, 1591, 1465, 1334, 1280,1178, 1126, 1029, 997, 864 cm⁻¹; MS (FAB) m/z 310(M+H)

B-39: C-(2-imidazol-1-yl-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 8.17 (d, 1H, J=7.9 Hz), 8.11 (s, 1H), 7.67 (d,1H, J=7.9 Hz), 7.49 (s, 1H), 7.14 (s, 1H), 3.93 (s, 2H); MS (FAB) m/z243 (M+H)

B-40:C-(4,6′-dimethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.45 (d, 1H, J=6.6 Hz), 6.75 (d, 1H, J=6.5 Hz), 3.80 (s, 2H), 3.30 (m,2H), 2.81 (m, 2H), 2.42 (s, 3H), 2.34 (bs, 2H), 1.72 (m, 2H), 1.51 (m,1H), 1.33 (m, 2H), 0.98 (d, 3H, J=5.7 Hz); IR (neat) 3364, 2919, 1580,1452, 1402, 1373, 1242, 1189, 1146, 1106, 1053, 962, 815 cm⁻¹; MS (FAB)m/z 220(M+H)

B-41: (3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-cyclohexyl-amine

¹H NMR (CDCl₃) δ 7.24 (d, 1H, J=7.4 Hz), 6.78 (d, 1H, J=7.1 Hz), 6.69(bs, NH), 3.99 (m, 1H), 3.84 (s, 2H), 2.09-2.01 (m, 2H), 1.75-1.21 (m,8H)

B-42:3′-aminomethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-ol

¹H NMR (CDCl₃) δ 7.90 (d, 1H, J=7.7 Hz), 7.35 (d, 1H, J=7.7 Hz), 3.90(s, 2H), 3.81-3.75 (m, 1H), 3.43-3.39 (m, 2H), 2.01-1.95 (m, 3H),1.72-1.61 (m, 2H)

B-43:6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylamine

¹H NMR (CDCl₃) δ 7.17 (d, 1H, J=8.0 Hz), 6.92 (d, 1H, J=8.0 Hz), 4.02(bs, NH), 3.07 (m, 4H), 1.74-1.56 (m, 6H); IR (neat) 2936, 1610, 1480,1428, 1374, 1320, 1277, 1172, 1121 cm⁻¹

B-44: (3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-butyl-amine

¹H NMR (CDCl₃) δ 7.24 (dd, 1H, J=7.3, 0.7 Hz), 6.80 (d, 1H, J=7.3 Hz),6.78 (br, NH), 3.86 (s, 2H), 3.50-3.44 (m, 2H), 1.67-1.57 (m, 2H),1.49-1.37 (m, 2H), 0.96 (t, 3H, J=7.1 Hz); IR (neat) 3301, 2929, 1611,1532, 1458, 1309, 1175, 1133, 817 cm⁻¹

B-45:C-[2-(6-aza-spiro[2.5]oct-6-yl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (CDCl₃) δ 7.82 (d, 1H, J=7.5 Hz), 7.26 (d, 1H, J=7.7 Hz), 3.93(s, 2H), 3.22 (m, 4H), 1.52 (m, 4H), 0.36 (s, 4H); IR (neat) 2923, 1593,1457, 1419, 1332, 1176, 1136, 956 cm⁻¹

B-46:C-(3-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (CDCl₃) δ 7.80 (dd, 1H, J=7.7, 0.7 Hz), 7.25 (d, 1H, J=7.5 Hz),3.90 (s, 2H), 3.41-3.33 (m, 2H), 2.84-2.75 (m, 1H), 2.54-2.47 (m, 1H),1.85-1.63 (m, 4H), 1.16-1.03 (m, 1H), 0.94 (d, 3H, J=6.6 Hz); IR (neat)2927, 1593, 1458, 1418, 1176, 1136, 1001 cm⁻¹

B-47:C-(2-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (CDCl₃) δ 8.05 & 7.78 (d, 1H), 7.65 & 7.32 (d, 1H), 4.04 & 3.78(m, 2H), 3.54 (m, 1H), 3.07 (m, 1H), 2.87 (m, 1H), 1.84-1.42 (m, 6H),0.96 (d, 3H, J=6.2 Hz); IR (neat) 2933, 1539, 1459, 1412, 1337, 1178,1139, 843 cm⁻¹

B-48:4[(3-aminomethyl-6-trifluoromethyl-pyridin-2-ylamino)-methyl]-piperidine-1-carbonicacid tert-butyl ester

¹H NMR (CDCl₃) δ 7.26 (m, 2H), 6.79 (d, 1H, J=7.0 Hz), 4.11 (m, 2H),3.89 (s, 2H), 3.39 (m, 2H), 2.69 (m, 2H), 1.85-1.65 (m, 5H), 1.43 (s,9H); IR (neat) 3376, 2925, 1680, 1610, 1533, 1427, 1366, 1173, 1137 cm⁻¹

B-49:C-(4-benzyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.80 (d, 1H, J=7.7 Hz), 7.35-7.21 (m, 6H), 3.88 (s, 2H), 3.45 (m, 2H),2.82 (m, 2H), 2.60 (d, 2H, J=6.6 Hz), 1.77-1.67 (m, 3H), 1.42 (m, 2H);IR (neat) 3385, 2921, 2847, 1592, 1454, 1418, 1373, 1320, 1267, 1174,1134, 953, 834, 746, 701 cm⁻¹; MS (FAB) m/z 350 (M+H)

B-50:C-{2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-yl}-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.84 (d, 1H, J=8.0 Hz), 7.31 (d, 1H, J=7.6Hz), 7.05-6.91 (m, 4H), 4.42 (s, 2H), 3.44-3.35 (m, 4H), 3.32-3.24 (m,4H), 1.57 (bs, 2H); IR (neat) 2844, 1591, 1510, 1418, 1334, 1232, 1176,1137, 1051, 966, 916, 825, 757 cm⁻¹; MS (FAB) m/z 355 (M+H)

B-51:C-{2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-yl}-methylamine

¹H NMR (300 MHz, CDCl₃)

7.87 (d, 1H, J=7.7 Hz), 7.31 (d, 1H, J=7.7 Hz), 7.21-7.03 (m, 4H), 3.96(s, 2H), 3.48-3.35 (m, 4H), 3.29-3.15 (m, 4H)

IR (neat) 3384m 2842m 1571m 1501m 1453, 1416, 1372, 1337, 1236, 1176,1136, 1052, 966, 822, 835, 754 cm⁻¹; MS (FAB) m/z 355 (M+H)

B-52:C-[2-(4-phenyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.88 (d, 1H, J=7.7 Hz), 7.35-7.26 (m, 3H),6.98 (d, 2H, J=7.9 Hz), 6.89 (m, 1H), 3.97 (s, 2H), 3.44-3.32 (m, 8H)

IR (neat) 2843, 1595, 1500, 1418, 1335, 1232, 1177, 1134, 966, 836, 759,693 cm⁻¹; MS (FAB) m/z 337 (M+H)

B-53: (3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-methyl-phenyl-amine

¹H NMR (300 MHz, CDCl₃)

7.83 (d, 1H, J=7.5 Hz), 7.34 (d, 1H, J=7.7 Hz), 7.26 (m, 2H), 7.05 (m,1H), 6.91 (m, 2H), 3.46 (s, 3H), 3.31 (s, 2H), 1.28 (bs, 2H); IR (neat)2915, 1588, 1496, 1465, 1396, 1349, 1264, 1180, 1137, 930, 835, 756, 699cm⁻¹; MS (FAB) m/z 282 (M+H)

B-54:C-(4,4-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.81 (d, 1H, J=7.7 Hz), 7.25 (d, 1H, J=7.8 Hz), 3.89 (s, 2H), 3.22-3.13(m, 4H), 1.59-1.46 (m, 4H), 1.01 (s, 6H); IR (neat) 2919, 1639, 1590,1459, 1423, 1375, 1321, 1252, 1175, 1138, 1047, 954, 835 cm⁻¹; MS (FAB)m/z 288 (M+H)

B-55: 2-(4-p-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.51 (d, 1H, J=9.0 Hz), 7.37 (d, 1H, J=6.4Hz), 7.36 (s, 1H), 7.11 (d, 2H, J=8.4 Hz), 6.90 (d, 2H, J=8.4 Hz), 3.99(s, 2H), 3.10-3.02 (m, 4H), 3.17-3.07 (m, 4H), 2.29 (s, 3H); IR (neat)2826, 1616, 1515, 1425, 1334, 1308, 1232, 1165, 1123, 1079, 959, 814cm⁻¹; MS (FAB) m/z 350 (M+H)

B-56: 2-(4-m-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.51 (d, 1H, J=7.5 Hz), 7.37 (d, 1H, J=7.7 Hz), 7.36 (s, 1H), 7.19 (m,1H), 6.81 (s, 1H), 6.80 (d, 1H, J=7.1 Hz), 6.73 (d, 1H, J=7.5 Hz), 3.99(s, 2H), 3.51-3.42 (m, 4H), 3.17-3.06 (m, 4H), 2.34 (s, 3H), 1.67 (bs,2H); IR (neat) 2828, 1604, 1498, 1425, 1336, 1310, 1250, 1166, 1123,962, 777 cm⁻¹; MS (FAB) m/z 350 (M+H)

B-57:4-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.59-7.42 (m, 3H), 7.38 (d, 1H, J=8.4 Hz), 7.35 (s, 1H), 6.99 (d, 2H,J=8.8 Hz), 4.00 (s, 2H), 3.49-3.35 (m, 4H), 3.19-3.05 (m, 4H); IR (neat)2838, 1616, 1527, 1425, 1332, 1238, 1163, 1116, 1073, 960, 827 cm⁻¹; MS(FAB) m/z 404 (M+H)

B-58:2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.50 (d, 1H, J=8.0 Hz), 7.38 (d, 1H, J=7.6Hz), 7.36 (s, 1H), 6.99-6.83 (m, 4H), 3.98 (s, 2H), 3.79 (s, 3H),3.29-3.18 (m, 4H), 3.17-3.04 (m, 4H); IR (neat) 3395, 2831, 1511, 1426,1307, 1244, 1167, 1123, 1078, 1037, 959, 826 cm⁻¹; MS (FAB) m/z 366(M+H)

B-59:2-[4-(4-fluoro-phenyl)-piperidin-1-yl]-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.48 (d, 1H, J=8.0 Hz), 7.35 (s, 1H), 7.34 (d, 1H, J=7.6 Hz), 7.24 (m,2H), 7.02 (m, 2H), 3.98 (s, 2H), 3.21 (bd, 2H, J=11.5 Hz), 2.86 (td, 2H,J=11.4, 2.9 Hz), 2.65 (m, 1H), 1.99-1.83 (m, 4H); IR (neat) 2921, 1608,1509, 1425, 1321, 1224, 1164, 1123, 1079, 949, 884, 833, 732 cm⁻¹; MS(FAB) m/z 353 (M+H)

B-60:C-(6″-trifluoromethyl-3,4,5,6,3′,4′,5′,6′-octahydro-2H,2′H-[1,4′;1′,2″]terpyridin-3″-yl)-methylamine

¹H NMR (300 MHz, CD₃OD)

7.91 (d, 1H, J=7.9 Hz), 7.35 (d, 1H, J=7.7 Hz), 3.87 (s, 2H), 3.52-3.56(m, 2H), 2.82-2.90 (m, 2H), 2.49-2.64 (m, 5H), 1.97-2.01 (m, 2H),1.50-1.51 (m, 8H); IR (neat) 2933, 2852, 1592, 1457, 14201339, 1135, 956cm⁻¹; MS (FAB) m/z 343 (M+H)

B-61:C-(4-pyrrolidin-1-yl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CD₃OD)

7.92 (d, 1H, J=7.7 Hz), 7.36 (d, 1H, J=7.7 Hz), 3.90 (s, 2H), 3.48-3.56(m, 2H), 2.87-2.95 (m, 2H), 2.72-2.83 (m, 5H), 2.42 (m, 1H), 2.03-2.15(m, 2H), 1.79-7.92 (m, 5H); IR (neat) 2959, 1592, 1459, 1421, 1339,1240, 1176, 1135, 957, 834 cm⁻¹; MS (FAB) m/z 329(M+H)

B-62:C-[6-(chloro-difluoro-methyl)-2-(4-phenyl-piperazin-1-yl)-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=7.5 Hz), 7.26-7.34 (m, 3H), 6.95-7.03 (m, 2H), 6.89 (m,1H), 3.96 (s, 2H), 3.30-3.46 (m, 8H); IR (neat) 2842, 1594, 1500, 1415,1375, 1231, 1091, 980, 932, 900, 817, 759, 682 cm⁻¹; MS (FAB) m/z 353(M+H)

B-63: 2-(4-phenyl-piperazin-1-yl)-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.50 (d, 1H, J=8.3 Hz), 7.24-7.39 (m, 4H),6.98 (d, 2H, J=8.1 Hz), 6.90 (dd, 1H, J=7.1, 7.1 Hz), 3.99 (s, 2H),3.22-3.37 (m, 4H), 3.08-3.13 (m, 4H); IR (neat) 2826, 1599, 1500, 1423,1334, 1308, 1232, 1163, 1121, 1079, 959, 882, 830, 760, 693 cm⁻¹; MS(FAB) m/z 336 (M+H)

B-64: 2-azocan-1-yl-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.46 (d, 1H, J=7.9 Hz), 7.41 (s, 1H), 7.30 (d,1H, J=8.0 Hz), 4.03 (s, 2H), 3.02-3.14 (m, 4H), 2.44-2.56 (m, 3H),1.61-1.81 (m, 7H); IR (neat) 2925, 1597, 1505, 1419, 1317, 1212, 1164,1123, 1080, 982, 907, 827 cm⁻¹; MS (FAB) m/z 287 (M+H)

B-65: 2-(4,4-dimethyl-piperidin-1-yl)-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.44 (d, 1H, J=7.9 Hz), 7.27-7.36 (m, 2H), 3.92 (s, 2H), 2.82-2.84 (m,4H), 1.46-1.60 (m, 4H), 1.01 (bs, 6H); IR (neat) 2919, 1424, 1337, 1309,1227, 1166, 1124, 1079, 949, 827, 734 cm⁻¹; MS (FAB) m/z 287 (M+H)

B-66: (2-aminomethyl-5-trifluoromethyl-phenyl)-dipropyl-amine

¹H NMR (300 MHz, CDCl₃) δ 7.47 (d, 1H, J=7.7 Hz), 7.31-7.37 (m, 2H),4.01 (s, 2H), 2.83-2.92 (m, 4H), 1.38-1.51 (m, 4H), 0.81-0.92 (m, 6H);IR (neat) 2964, 2875, 1463, 1422, 1327, 1220, 1166, 1125, 1079, 984, 891cm⁻¹; MS (FAB) m/z 275 (M+H)

B-67: 4-trifluoromethyl-2-(4-trifluoromethyl-piperidin-1-yl)-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.50 (d, 1H, J=8.1 Hz), 7.36 (d, 1H, J=7.7 Hz), 7.29 (bs, 1H), 3.95 (s,2H), 3.14-3.25 (m, 2H), 2.67-2.80 (m, 2H), 2.20 (m, 1H), 1.93-2.05 (m,2H), 1.75-1.87 (m, 2H); IR (neat) 2958, 2820, 1424, 1333, 1306, 1254,1128, 1081, 949, 899, 829, 734 cm⁻¹; MS (FAB) m/z 327 (M+H)

B-68:3′-aminomethyl-4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-5′-carbonicacid ethyl ester

¹H NMR (300 MHz, CDCl₃) δ 8.13 (s, 1H), 4.37 (q, 2H, J=7.1 Hz), 3.88 (s,2H), 3.69 (m, 2H), 2.90 (t, 2H, J=11.5 Hz), 1.67 (m, 3H), 1.32 (m, 5H),0.95 (d, 3H, J=13.7 Hz); IR (neat) 3391, 2924, 1542, 1452, 1373, 1024,971, 794 cm⁻¹; MS (FAB) m/z 346(M+H)

B-69:C-[6′-(chloro-difluoro-methyl)-3,5-dimethyl-3,4,5,6-tetrahydro-2H[1,2′]bipyridinyl-3′-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.75 (d, 1H, J=7.5 Hz), 7.18 (d, 1H, J=7.7 Hz), 3.89 (s, 2H), 3.18 (tt,4H, J=7.3, 2.0 Hz), 1.60-1.48 (m, 4H), 0.86 (t, 6H, J=7.3 Hz); IR (neat)3033, 2935, 1726, 1594, 1514, 1456, 1420 cm⁻¹; MS (FAB) m/z 304 (M+H)

B-70: (3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-dipropyl-amine

¹H NMR (300 MHz, CDCl₃)

7.75 (d, 1H, J=7.5 Hz), 7.18 (d, 1H, J=7.7 Hz), 3.89 (s, 2H), 3.18 (tt,4H, J=7.3, 2.0 Hz), 1.60-1.48 (m, 4H), 0.86 (t, 6H, J=7.3 Hz); IR (neat)3367, 2966, 2875, 1593, 1465, 1419, 1338 cm⁻¹; MS (FAB) m/z 261 (M+H)

B-71:C-(6′-tert-butyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.48 (d, 1H, J=7.7 Hz), 6.90 (d, 1H, J=7.7Hz), 3.83 (s, 2H), 3.08 (m, 4H), 1.70-1.50 (m, 6H), 1.30 (s, 9H); IR(neat) 2933, 2856, 1635, 1582, 1445, 1402, 1370 cm⁻¹; MS (FAB) m/z 248(M+H)

B-72: C-(6-tert-butyl-2-pyrrolidin-1-yl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.36 (d, 1H, J=7.5 Hz), 6.70 (d, 1H, J=7.7 Hz), 3.86 (s, 2H), 3.53 (m,4H), 1.96-1.90 (m, 4H), 1.30 (s, 9H); IR (neat) 2959, 2866, 1583, 1450,1355, 1251, 1099 cm⁻¹; MS (FAB) m/z 234 (M+H)

B-73:C-(6′-tert-butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.48 (d, 1H, J=7.7 Hz), 6.90 (d, 1H, J=7.9 Hz), 3.86 (s, 2H), 3.36 (m,2H), 2.82 (m, 2H), 1.70-1.67 (m, 2H), 1.57-1.31 (m, 3H), 1.30 (s, 9H),0.98 (d, 3H, J=6.4 Hz); IR (neat) 2954, 2921, 2869, 1635, 1583, 1451,1403 cm⁻¹; MS (FAB) m/z 262 (M+H)

B-74: C-(2-azepan-1-yl-6-tert-butyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.40 (d, 1H, J=7.7 Hz), 6.76 (d, 1H, J=7.7 Hz), 3.82 (s, 2H), 3.49-3.42(m, 4H), 1.80 (m, 4H), 1.62 (m, 4H), 1.30 (s, 9H); IR (neat) 3396, 2925,2856, 1643, 1582, 1454, 1364 cm⁻¹; MS (FAB) m/z 262 (M+H)

B-75:C-(6′-tert-butyl-4-phenyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.52 (d, 1H, J=7.7 Hz), 7.36-7.19 (m, 5H), 6.95 (d, 1H, J=7.7 Hz), 3.88(s, 2H), 3.55-3.51 (m, 2H), 3.48 (s, 3H), 3.03-2.93 (m, 2H), 2.75-2.64(m, 1H), 2.05-1.54 (m, 4H), 1.33 (s, 9H); IR (neat) 2957, 1644, 1578,1452, 1401, 1370, 1231 cm⁻¹; MS (FAB) m/z 324 (M+H)

B-76: (3-aminomethyl-6-tert-butyl-pyridin-2-yl)-dipropyl-amine

¹H NMR (300 MHz, CDCl₃)

7.45 (d, 1H, J=7.7 Hz), 6.94 (d, 1H, J=7.7 Hz), 3.99 (s, 2H), 3.25-3.05(m, 4H), 1.61-1.38 (m, 4H), 1.33 (s, 9H), 0.90-0.80 (m, 6H); IR (neat)2961, 2871, 1634, 1583, 1460, 1369, 1243 cm⁻¹; MS (FAB) m/z 264 (M+H)

B-77: (3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-diethyl-amine

¹H NMR (300 MHz, CDCl₃)

7.67 (d, 1H, J=7.5 Hz), 7.07 (d, 1H, J=7.7 Hz), 3.79 (s, 2H), 3.20-3.09(q, 4H, J=7.0 Hz), 0.98 (t, 4H, J=7.0 Hz); IR (neat) 2924, 1588, 1429,1332, 1219, 1170, 1129 cm⁻¹; MS (FAB) m/z 248 (M+H)

B-78: (3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-di methyl-amine

¹H NMR (300 MHz, CDCl₃) δ 7.72 (d, 1H, J=7.5 Hz), 7.12 (d, 1H, J=7.5Hz), 4.01 (s, 2H), 2.85 (s, 4H); IR (neat) 2923, 1596, 1488 1394, 1350,1272, 1175 cm⁻¹; MS (FAB) m/z 219 (M+H)

B-79: (3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-benzyl-amine

¹H NMR (300 MHz, CDCl₃)

7.29-7.10 (m, 6H), 6.70 (d, 1H, J=7.4 Hz), 4.54 (d, 1H, J=2.0 Hz), 3.66(s, 2H), 1.41 (bs, 2H); IR (neat) 3298, 2920, 1609, 1530, 1453, 13541309 cm⁻¹; MS (FAB) m/z 282 (M+H)

B-80:C-(4,4′-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.17 (s, 1H), 4.09 (s, 2H), 3.31 (m, 2H), 2.89 (m, 2H), 2.43 (s, 3H),1.76 (m, 2H), 1.53 9m, 1H), 1.37 (m, 2H), 1.44 (bs, 2H), 0.98 (d, 3H,J=6.3 Hz); IR (neat) 3380, 2952, 1598, 1567, 1465, 1373, 1311, 1276,1176, 1138, 968, 916 cm⁻¹; MS (FAB) m/z 288(M+H)

Method 3:

Compounds of the general formula VI-B (1.5 mmol), in which R⁵, R¹², R¹³,U, T and V have the above-stated meaning and m denotes 0, 1, 2 or 3, aredissolved in diethylether (3 mL) and a suspension of lithium aluminiumhydride (3 mmol) in diethylether (5 mL) is slowly added. The reactionmixture is heated to reflux for 4 hours, and methanol and 1 N aq. NaOHsoln. are slowly added at 0° C. The reaction mixture is diluted withmethanol and filtered over celite. The solvent is evaporated under avacuum and the residue is purified by flash chromatography (SiO₂,different mixtures of methylene chloride and methanol).

The following compound B-81 was prepared according to the above-statedprocedure.

B-81:C-(4-methylene-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (CDCl₃) δ 7.84 (d, 1H, J=7.7 Hz), 7.27 (d, 1H, J=7.0 Hz), 4.76(s, 2H), 3.94 (s, 2H), 3.25 (t, 4H, J=5.7 Hz), 2.38 (t, 4H, J=5.7 Hz)

Method 4:

Compounds of the general formula VI-B (0.39 mmol), in which R⁵, R¹²,R¹³, U, T and V have the above-stated meaning and m denotes 0, 1, 2 or3, are dissolved in methanol (8 mL) and NiCl₂.H₂O (0.78 mmol) and sodiumborohydride (1.56 mmol) are slowly added at 0° C. The reaction mixtureis heated to reflux for 12 hours. The reaction mixture is diluted withmethanol and filtered over celite. The solvent is evaporated under avacuum and the residue is purified by flash chromatography (SiO₂,different mixtures of methylene chloride and methanol).

The following compounds B-82 to B-84 were obtained according to theabove-stated general method:

B-82: (3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-butyl-methyl-amine

¹H NMR (300 MHz, CDCl₃) δ 7.75 (d, 1H, J=7.5 Hz), 7.18 (d, 1H, J=7.7Hz), 3.91 (bs, 2H), 3.19 (bt, 2H), 2.89 (bs, 3H), 1.52-1.65 (m, 2H),1.21-1.39 (m, 2H), 0.92 (t, 3H, J=7.3 Hz); IR (neat) 2961, 2868, 1594,1465, 1400, 1334, 1176, 1136, 831 cm⁻¹; MS (FAB) m/z 262 (M+H)

B-83:C-(4-phenyl-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.85 (d, 1H, J=7.5 Hz), 7.43 (d, 1H, J=7.5 Hz), 7.22-7.35 (m, 5H), 6.20(m, 1H), 3.97-4.01 (m, 4H), 3.41-3.46 (m, 4H), 2.74 (bs, 2H); IR (neat)3395, 2922, 1593, 1422, 1372, 1338, 1267, 1175, 1135, 959, 833, 750, 697cm⁻¹; MS (FAB) m/z 334(M+H)

B-84:C-[4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=7.8 Hz), 7.40 (m, 3H), 7.03 (dd, 2H, J=9.0, 8.3 Hz), 6.14(bs, 1H), 3.97-4.01 (m, 4H), 3.46 (m, 2H), 2.70 (m, 2H), 1.82 (bs, 2H);IR (neat) 3365, 2922, 1600, 1510, 1425, 1340, 1230, 1174, 1135, 963, 835cm⁻¹; MS (FAB) m/z 334(M+H)

3. General Procedure for the Preparation of Amines of General FormulaV-Ba and V-Bb

Amines of general formula V-Ba and VB-b are prepared as described inscheme 2. depicted below.

Stage 1: Preparation of Nitriles of General Formula VI-Ca and VI-Cb

Compounds of general formula VI-A (1 equivalent), wherein R⁵, U, T and Vhave the meaning as described above and m denotes 0, 1, 2 or 3, aretreated with an alcohol of general formula HO—R¹⁴ (3.5 equivalents) andDBU [1,8-diaza-bicyclo[5.4.0]andec-7-ene] (3.5 equivalents) inacetonitrile (7 mL per mmol of compound of general formula VI-A) for 12hours at room temperature. The reaction mixture is extracted repeatedlywith EA. The combined organic phases are washed with sat. aq. NaClsoln., dried over MgSO₄ and the solvent is removed under a vacuum. Theresidue is in each case purified via column chromatography (SiO₂,different mixtures of hexanes and EA).

Alternatively, compounds of general formula VI-Ca or VI-Cb (1equivalent), wherein R⁵, U, T and V have the meaning as described above,m denotes 0, 1, 2 or 3 and R¹⁴ or R¹⁵ denotes hydrogen, are treated witha compound of general formula R¹⁴—Br or R¹⁵—Br (4 equivalents), whereinR¹⁴ and R¹⁵ have the above-stated meaning and are different fromhydrogen, in a mixture of acetonitrile and dimethyl formamide (1:2),optionally in the presence of 18-crown-6-ether as catalyst. The reactionmixture was refluxed for 12 h and allowed to cool to room temperature.The mixture was extracted with EA (30 mL). The organic phase was driedover MgSO₄, filtered, and concentrated in vacuo. The residue waspurified by flash column chromatography on silica gel using EA/hexanes(1:1) as eluent.

The following compounds A-104 to A-173 were obtained according to theabove-stated general method:

A-104: 2-(3-methyl-butoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.05 (d, 1H, J=7.8 Hz), 7.33 (d, 1H, J=7.8 Hz), 4.53 (t, 2H, J=6.9 Hz),1.65-1.96 (m, 3H), 0.98 (d, 6H, J=6.3 Hz); MS (FAB) m/z 259 (M+H)

A-105: 2-(3,3-dimethyl-butoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.05 (d, 1H, J=7.8 Hz), 7.33 (d, 1H, J=7.8 Hz), 4.56 (t, 2H, J=6.9 Hz),1.77 (t, 2H, J=6.9 Hz), 1.01 (s, 9H); MS (FAB) m/z 273 (M+H)

A-106: 2-(2-methyl-cyclopropylmethoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.05 (d, 1H, J=7.8 Hz), 7.32 (d, 1H, J=7.8 Hz), 4.33 (m, 2H), 1.06 (d,3H, J=6.0 Hz), 1.02 (m, 1H), 0.85 (m, 1H), 0.56 (m, 1H), 0.46 (m, 1H);MS (FAB) m/z 257 (M+H)

A-107: 2-butoxy-6-(chloro-difiuoro-methyl)-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) d 8.02 (d, 1H, J=7.8 Hz), 7.28 (d, 1H, J 07.8Hz), 4.59 (t, 2H, J=7.2 Hz), 1.84 (m, 2H), 1.50 (m, 2H), 0.99 (t, 3H,J=6.9 Hz);

IR (KBr) 2964, 2210, 1590, 1432, 1373, 1325, 1190 cm⁻¹; MS (FAB) m/z 265(M+H)

A-108: 2-phenoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.18 (d, 1H, J=7.8 Hz), 7.41-7.47 (m, 2H), 7.21-7.31 (m, 4H); IR(neat)3100, 2950, 2210, 1580, 1490, 1462, 1411, 1194, 1271, 1150, 947 cm⁻¹; MS(FAB) m/z 265 (M+H)

A-109: 2-(1-butyl-pentyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.03 (d, 1H, J=7.8 Hz), 7.29 (d, 1H, J=7.8 Hz), 5.36 (m, 1H), 1.65-1.78(m, 4H), 1.32-1.39 (m, 8H), 0.90 (t, 6H, J=7.2 Hz)

IR (neat) 2960, 2867, 2236, 1590, 1463, 1434, 1347, 1265, 1186, 1152,1119, 966, 840, 743 cm⁻¹; MS (FAB) m/z 315 (M+H)

A-110: 2-(1-ethyl-propoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.96 (d, 1H, J=7.8 Hz), 7.29 (d, 1H, J=7.8 Hz), 5.15 (m, 1H), 1.72 (m,4H), 0.89 (t, 6H, J=6.8 Hz); IR(neat) 2974, 2236, 1590, 1462, 1435,1348, 1266, 1186, 1151, 1117, 967, 840 cm⁻¹; MS (FAB) m/z 259 (M+H)

A-111: 2-(1-propyl-butoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.04 (d, 1H, J=7.8 Hz), 7.20 (d, 1H, J=7.8 Hz), 5.41 (m, 1H), 1.69 (m,4H), 1.43 (m, 4H), 0.93 (t, 6H, J=6.9 Hz)

IR(neat) 2964, 2875, 2236, 1590, 1462, 1435, 1347, 1267, 1187, 1152,1119, 979, 839, 744 cm⁻¹; MS (FAB) m/z 287 (M+H)

A-112: 2-(1-isobutyl-3-methyl-butoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

7.97 (d, 1H, J=7.8 Hz), 7.23 (d, 1H, J=7.8 Hz), 5.49 (m, 1H), 1.60-1.78(m, 6H), 0.84 (d, 12H, J=6.9 Hz); IR(neat) 3365, 2958, 2871, 2237, 1590,1464, 1434, 1347, 1266, 1187, 1154, 964, 839 cm⁻¹; MS (FAB) m/z 315(M+H)

A-113: 2-(4,4-dimethyl-cyclohexyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.02 (d, 1H, J=7.8 Hz), 7.28 (d, 1H, J=7.8Hz), 5.21 (m, 1H), 1.73-1.96 (m, 4H), 1.55 (m, 2H), 1.33 (m, 2H), 0.99(s, 3H), 0.96 (s, 3H); MS (FAB) m/z 299 (M+H)

A-114: 2-(3-methoxy-propoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.06 (d, 1H, J=7.7 Hz), 7.35 (d, 1H, J=7.7Hz), 4.59 (t, 2H, J=6.2 Hz), 3.59 (t, 2H, J=6.1 Hz), 3.37 (s, 3H),2.07-2.17 (m, 2H); IR (neat) 2929, 2223, 1591, 1463, 1375, 1347, 1312,1267, 1188, 1150, 1119, 977, 922, 742 cm⁻¹; MS (FAB) m/z 261 (M+H)

A-115: 2-(3-ethoxy-propoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.34 (d, 1H, J=7.7Hz), 4.60 (t, 2H, J=6.2 Hz), 3.62 (d, 2H, J=6.2 Hz), 3.50 (q, 2H, J=7.5Hz), 2.04-2.16 (m, 2H), 1.99 (t, 3H, J=7.0 Hz); IR (neat) 2976, 2870,2237, 1590, 1470, 1436, 1375, 1347, 1269, 1187, 1150, 1118, 994, 842,743 cm⁻¹ MS (FAB) m/z 275 (M+H)

A-116: 2-(2-phenoxy-ethoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.07 (d, 1H, J=7.7 Hz), 7.38 (d, 1H, J=7.7Hz), 7.24-7.35 (m, 2H), 6.01-7.02 (m, 3H), 4.86 (t, 2H, J=5.0 Hz), 4.39(t, 2H, J=5.0 Hz); IR (neat) 2235, 1589, 1429, 1348, 1241, 1193, 1142,1112, 963, 840, 753, 692 cm⁻¹; MS (FAB) m/z 309 (M-FH)

A-117: 2-butoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (d, 1H, J=7.7 Hz), 7.33 (d, 1H, J=7.7 Hz), 4.50(t, 2H, J=6.6 Hz), 1.87-1.78 (m, 2H), 1.58-1.45 (m, 2H), 0.99 (t, 3H,J=7.3 Hz)

IR (neat) 2965, 2240, 1591, 1468, 1436, 1349, 1270, 1189, 1151 cm⁻¹

A-118: 2-isopropoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (d, 1H, J=7.7 Hz), 7.30 (d, 1H, J=7.7 Hz), 5.46(m, 1H), 1.43 (d, 6H, J=6.2 Hz)

IR (neat) 2988, 2237, 1591, 1435, 1343, 1269, 1187, 1150, 1115, 969 cm⁻¹

A-119: 2-cyclopentyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.02 (dd, 1H, J=7.7, 0.6 Hz), 7.30 (d, 1H, J=7.5 Hz),5.60-5.54 (m, 1H), 2.09-1.57 (m, 8H)

IR (neat) 2969, 2236, 1590, 1435, 1350, 1268, 1187, 1150, 974 cm⁻¹

A-120: 2-cyclohexyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.02 (d, 1H, J=7.7 Hz), 7.29 (d, 1H, J=7.7 Hz), 5.24(m, 1H), 2.03-1.95 (m, 2H), 1.87-1.40 (m, 8H); IR (neat) 2940, 2862,2236, 1591, 1436, 1348, 1269, 1188, 1150, 971 cm⁻¹

A-121: 2-methoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.06 (d, 1H, J=7.7 Hz), 7.37 (d, 1H, J=7.7 Hz), 4.13(s, 3H); IR (neat) 2924, 2238, 1592, 1475, 1392, 1349, 1272, 1186, 1149,1009 cm⁻¹

A-122: 2-hexyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (dd, 1H, J=7.7, 0.7 Hz), 7.33 (d, 1H, J=7.7 Hz),4.49 (t, 2H, J=6.6 Hz), 1.89-1.79 (m, 2H), 1.50-1.30 (m, 6H), 0.91 (t,3H); IR (neat) 2931, 1591, 1469, 1437, 1348, 1269, 1189, 1151 cm⁻¹

A-123: 2-isobutoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (d, 1H, J=7.7 Hz), 7.33 (d, 1H, J=7.7 Hz), 4.26(d, 1H, J=6.6 Hz), 2.17 (m, 1H), 1.06 (d, 6H, J=6.8 Hz); IR (neat) 2968,2237, 1592, 1469, 1436, 1347, 1268, 1188, 1151, 1119, 1000 cm⁻¹

A-124: 2-cyclopropylmethoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.33 (d, 1H, J=7.7 Hz), 4.35(d, 2H, J=7.1 Hz), 1.40-1.30 (m, 1H), 0.68-0.62 (m, 2H), 0.45-0.40 (m,2H); IR (neat) 2960, 2240, 1592, 1468, 1438, 1391, 1355, 1266, 1187,1149, 1119 cm⁻¹

A-125: 2-cyclobutylmethoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (d, 1H, J=7.7 Hz), 7.33 (d, 1H, J=7.7 Hz), 4.46(d, 2H, J=6.6 Hz), 2.88-2.78 (m, 1H), 2.20-1.85 (m, 6H); IR (neat) 2941,2238, 1591, 1469, 1435, 1349, 1269, 1188, 1150, 1117, 988 cm⁻¹

A-126: 2-propoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.05 (dd, 1H), 7.33 (d, 1H, J=7.7 Hz), 4.46 (t, 2H,J=6.6 Hz), 1.93-1.82 (m, 2H), 1.06 (t, 3H, J=7.5 Hz)

IR (neat) 2974, 2238, 1592, 1437, 1346, 1271, 1190, 1151, 979 cm⁻¹

A-127: 2-pentyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (dd, 1H), 7.33 (d, 1H, J=7.7 Hz), 4.49 (t, 2H,J=6.8 Hz), 1.89-1.80 (m, 2H), 1.51-1.35 (m, 4H), 0.94 (t, 3H, J=6.9 Hz);IR (neat) 2962, 2240, 1592, 1437, 1349, 1270, 1190, 1151 cm⁻¹

A-128: 2-cyclobutoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.03 (dd, 1H, J=7.7, 0.7 Hz), 7.32 (d, 1H, J=7.7 Hz),5.32 (m, 1H), 2.56-2.46 (m, 2H), 2.32-2.19 (m, 2H), 1.94-1.66 (m, 2H)

IR (neat) 2995, 2238, 1590, 1465, 1434, 1345, 1269, 1188, 1150 cm⁻¹

A-129: 2-(4-methyl-cyclohexyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.02 (d, 1H, J=7.7 Hz), 7.29 (d, 1H, J=7.7 Hz), 5.11(m, 1H), 2.20-2.12 (m, 2H), 1.85-1.75 (m, 2H), 1.63-1.43 (m, 3H),1.20-1.05 (m, 2H), 0.94 (d, 3H, J=6.6 Hz); IR (neat) 2950, 2238, 1591,1462, 1436, 1350, 1267, 1187, 1151, 993 cm⁻¹

A-130: 2-cyclopentylmethoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (dd, 1H, J=7.7, 0.5 Hz), 7.33 (d, 1H, J=7.7 Hz),4.37 (d, 2H, J=6.9 Hz), 2.43 (m, 1H), 1.91-1.81 (m, 2H), 1.71-1.56 (m,4H), 1.45-1.34 (m, 2H); IR (neat) 2957, 2236, 1592, 1436, 1346, 1269,1188, 1150, 988 cm⁻¹

A-131: 2-ethoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.33 (d, 1H, J=7.7 Hz), 4.57(q, 2H, J=7.0 Hz), 1.47 (t, 3H, J=7.0 Hz); IR (neat) 2990, 2238, 1591,1437, 1389, 1348, 1269, 1189, 1150, 1024 cm⁻¹

A-132: 2-(4-tert-butyl-cyclohexyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.02 (d, 1H, J=7.7 Hz), 7.29 (d, 1H, J=7.7 Hz), 5.07(m, 1H), 2.24-2.20 (m, 2H), 1.92-1.85 (m, 2H), 1.60-1.46 (m, 2H),1.27-1.04 (m, 3H), 0.89 (s, 9H); IR (neat) 2954, 2237, 1591, 1435, 1350,1269, 1188, 1151, 977 cm⁻¹

A-133: 2-(4-ethyl-cyclohexyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.02 (d, 1H, J=7.0 Hz), 7.29 (d, 1H, J=7.7 Hz), 5.11(m, 1H), 2.21-2.13 (m, 2H), 1.92-1.85 (m, 2H), 1.62-1.03 (m, 7H), 0.91(t, 3H, J=7.0 Hz); IR (neat) 2934, 2237, 1591, 1435, 1350, 1269, 1188,1151 cm⁻¹

A-134: 6-tert-butyl-2-cyclohexyloxy-nicotinonitrile

¹H NMR (CDCl₃) δ 7.76 (d, 1H, J=7.9 Hz), 6.91 (d, 1H, J=7.9 Hz), 5.16(m, 1H), 2.03-1.35 (m, 10H), 1.32 (s, 9H); IR (neat) 2938, 2230, 1592,1564, 1451, 1415, 1365, 1261 cm⁻¹

A-135: 6-tert-butyl-2-cyclopentyloxy-nicotinonitrile

¹H NMR (CDCl₃) δ 7.75 (d, 1H, J=7.9 Hz), 6.91 (d, 1H, J=7.9 Hz), 5.50(m, 1H), 2.03-1.60 (m, 8H), 1.32 (s, 9H); IR (neat) 2964, 2230, 1592,1564, 1451, 1414, 1353, 1262, 984 cm⁻¹

A-136: 2-butoxy-6-tert-butyl-nicotinonitrile

¹H NMR (CDCl₃) δ 7.77 (d, 1H, J=7.9 Hz), 6.94 (d, 1H, J=7.9 Hz), 4.44(t, 2H, J=6.6 Hz), 1.80 (m, 2H), 1.49 (m, 2H), 1.32 (s, 9H), 0.98 (t,3H, J=7.3 Hz); IR (neat) 2961, 2230, 1593, 1565, 1455, 1418, 1369, 1261,1112 cm⁻¹

A-137: 6-tert-butyl-2-hexyloxy-nicotinonitrile

¹H NMR (CDCl₃) δ 7.77 (d, 1H, J=7.9 Hz), 6.94 (d, 1H, J=7.9 Hz), 4.43(t, 2H, J=6.8 Hz), 1.81 (m, 2H), 1.50-1.30 (m, 6H), 1.32 (s, 9H), 0.90(m, 3H);

IR (neat) 2929, 2230, 1593, 1565, 1455, 1418, 1369, 1261, 1112, 1000cm⁻¹

A-138: 2-benzyloxy-6-tert-butyl-nicotinonitrile

¹H NMR (CDCl₃) δ 7.79 (d, 1H, J=8.3 Hz), 7.50-7.30 (m, 5H), 6.97 (d, 1H,J=7.9 Hz), 5.53 (s, 2H), 1.31 (s, 9H); IR (neat) 2963, 2230, 1593, 1563,1454, 1412, 1360, 1263, 1114, 999 cm⁻¹

A-139: 2-cyclohexylmethoxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (d, 1H, J=7.9 Hz), 7.32 (d, 1H, J=7.7 Hz), 4.28(d, 2H, J=6.0 Hz), 1.90-1.70 (m, 6H), 1.35-1.05 (m, 5H); IR (neat) 2930,2237, 1592, 1438, 1349, 1268, 1188, 1151, 994 cm⁻¹

A-140: 2-(4-methyl-cyclohexylmethoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (CDCl₃) δ 8.04 (d, 1H, J=7.7 Hz), 7.32 (d, 1H, J=7.7 Hz), 4.40 &4.29 (d, 2H), 2.06-1.50 (m, 7H), 1.37-1.28 (m, 2H), 1.15-1.05 (m, 1H),0.95 & 0.90 (d, 3H);

IR (neat) 2924, 2237, 1592, 1437, 1349, 1268, 1188, 1151, 1118, 988 cm⁻¹

A-141:4-(3-cyano-6-trifluoromethyl-pyridin-2-yloxymethyl)-piperidine-1-carbonicacid tert-butyl ester

¹H NMR (CDCl₃) δ 8.06 (d, 1H, J=7.7 Hz), 7.36 (d, 1H, J=7.7 Hz), 4.34(d, 2H), 4.23-4.12 (m, 2H), 2.81-2.70 (m, 2H), 2.04 (m, 1H), 1.87-1.81(m, 2H), 1.47 (s, 9H), 1.37-1.23 (m, 2H); IR (neat) 2926, 2236, 1690,1591, 1434, 1363, 1268, 1181, 1149, 986 cm⁻¹

A-142:6-trifluoromethyl-2-(4-trifluoromethyl-cyclohexyloxy)-nicotinonitrile

¹H NMR (CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.34 (d, 1H, J=7.7 Hz), 5.51 &5.14 (m, 1H), 2.35-2.05 (m, 4H), 1.87-1.50 (m, 5H); IR (neat) 2957,2237, 1591, 1463, 1436, 1346, 1270, 1186, 1150, 1014 cm⁻¹

A-143:4-(3-cyano-6-trifluoromethyl-pyridin-2-yloxy)-piperidine-1-carbonic acidtert-butyl ester

¹H NMR (CDCl₃) δ 8.07 (d, 1H, J=7.7 Hz), 7.35 (d, 1H, J=7.7 Hz), 5.42(m, 1H), 3.73 (m, 2H), 3.43 (m, 2H), 2.05-1.83 (m, 4H), 1.48 (s, 9H); IR(neat) 2975, 2237, 1693, 1591, 1430, 1350, 1273, 1236, 1181, 1022 cm⁻¹

A-144: 2-(3-methoxy-benzyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.06 (d, 1H, J=7.7 Hz), 7.36 (d, 1H, J=7.7 Hz), 7.29 (d, 1H, J=7.7 Hz),7.10 (d, 1H, J=7.9 Hz), 7.09 (s, 1H), 6.88 (m, 1H), 5.54 (s, 2H), 3.82(s, 3H); IR (neat) 2920, 2228, 1591, 1463, 1428, 1350, 1269, 1149, 980,843, 781 cm⁻¹; MS (FAB) m/z 309 (M+H)

A-145: 2-(4-methyl-benzyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.42 (d, 2H, J=8.0Hz), 7.32 (d, 1H, J=7.7 Hz), 7.19 (d, 2H, J=7.9 Hz), 5.52 (s, 2H), 2.36(s, 3H)

IR (neat) 2923, 2236, 1590, 1464, 1432, 1348, 1270, 1186, 1149, 1117,977, 842, 808, 745 cm⁻¹; MS (FAB) m/z 293 (M+H)

A-146: 2-(4-fluoro-benzyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.07H, J=7.7 Hz), 7.52 (m, 2H), 7.37 (d, 1H,J=7.7 Hz), 7.07 (m, 2H), 5.52 (s, 2H); IR (neat) 2230, 1590, 1512, 1465,1434, 1348, 1270, 1228, 1187, 1151, 1116, 979, 835, 745 cm⁻¹; MS (FAB)m/z 297 (M+H)

A-147: 2-(pyridin-4-ylmethoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.66 (s, 2H), 8.13 (d, 1H, J=7.7 Hz),7.48-7.39 (m, 3H), 5.57 (s, 2H); IR (neat) 3028, 2218, 1591, 1466, 1427,1358, 1275, 1176, 1145, 1021, 1145, 1021, 938, 865, 801, 772 cm⁻¹; MS(FAB) m/z 280 (M+H)

A-148: 2-phenethyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.03 (d, 1H, J=7.7 Hz), 7.41-7.26 (m, 6H),4.67 (t, 2H, J=6.9 Hz), 3.15 (t, 2H, J=6.9 Hz); IR (neat) 3031, 2236,1590, 1468, 1434, 1348, 1268, 1187, 1148, 1117, 996, 955, 842, 749, 701cm⁻¹; MS (FAB) m/z 293 (M+H)

A-149: 2-(pyridin-2-ylmethoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.62 (m, 1H), 8.11 (d, 1H, J=7.7 Hz), 7.76 (td, 1H, J=7.7, 1.8 Hz), 7.57(d, 1H, J=7.7 Hz), 7.41 (d, 1H, J=7.7 Hz), 7.27 (m, 1H), 5.66 (s, 2H);IR (neat) 2237, 1588, 1473, 1423, 1355, 1279, 1191, 1149, 1024, 937,857, 768 cm⁻¹; MS (FAB) m/z 280 (M+H)

A-150: 2-benzyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.06 (d, 1H, J=7.7 Hz), 7.58-7.50 (m, 2H),7.47-7.36 (m, 4H), 5.56 (s, 2H); IR (neat) 2237, 1590, 1464, 1429, 1350,1271, 1180, 1149, 1115, 984, 842, 741, 699 cm⁻¹; MS (FAB) m/z 279 (M+H)

A-151: 2-benzyloxy-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃)

7.72 (d, 1H, J=7.9 Hz), 7.48-7.34 (m, 5H), 7.29 (d, 1H, J=8.0 Hz), 7.25(s, 1H), 5.26 (s, 2H); IR (neat) 2229, 1504, 1431, 1371, 1328, 1243,1121, 1078, 991, 877, 822, 738, 695 cm⁻¹; MS (FAB) m/z 278 (M+H)

A-152: 2-(pyridin-3-ylmethoxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.78 (s, 1H), 8.61 (d, 1H, J=4.8 Hz), 8.09 (d, 1H, J=7.7 Hz), 7.88 (dt,1H, J=7.9 Hz), 7.39 (d, 1H, J=7.7 Hz), 7.34 (m, 1H), 5.58 (s, 2H); IR(neat) 2231, 1587, 1411, 1348, 1269, 1175, 1110, 1014, 936, 847, 790,707 cm⁻¹; MS (FAB) m/z 280 (M+H)

A-153: 6-trifluoromethyl-2-(4-trifluoromethyl-benzyloxy)-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.09 (d, 1H, J=7.6 Hz), 7.76-7.61 (m, 4H),7.39 (d, 1H, J=7.8 Hz), 5.61 (s, 2H); IR (neat) 2237, 1590, 1466, 1434,1326, 1272, 1121, 1067, 1012, 845, 744 cm⁻¹; MS (FAB) m/z 347 (M+H)

A-154: 2-(4-ethyl-benzyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.04 (d, 1H, J=7.7 Hz), 7.45 (d, 2H, J=7.9Hz), 7.34 (d, 1H, J=7.7 Hz), 7.22 (d, 2H, J=8.0 Hz), 5.53 (s, 2H), 2.66(q, 2H, J=7.7 Hz), 1.24 (t, 3H, J=7.6 Hz); IR (neat) 2967, 2231, 1590,1464, 1432, 1348, 1271, 1187, 1150, 1117, 977, 843 cm⁻¹; MS (FAB) m/z307 (M+H)

A-155: 2-(4-butyl-benzyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.43 (d, 2H, J=7.9Hz), 7.34 (d, 1H, J=7.7 Hz), 7.20 (d, 2H, J=7.9 Hz), 5.52 (s, 2H), 2.61(t, 2H, J=7.7 Hz), 1.60 (m, 2H), 1.35 (m, 2H), 0.92 (t, 3H, J=7.3 Hz);IR (neat) 2930, 2230, 1590, 1464, 1432, 1348, 1271, 1187, 1150, 1116,976, 840 cm⁻¹; MS (FAB)) m/z 335 (M+H)

A-156: 2-(4-tert-butyl-benzyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.05 (d, 1H, J=7.6 Hz), 7.57-7.40 (m, 4H),7.35 (d, 1H, J=7.8 Hz), 5.53 (s, 2H), 1.33 (s, 9H); IR (neat) 2964,2237, 1590, 1465, 1432, 1348, 1271, 1186, 1150, 1117, 975, 840, 744cm⁻¹; MS (FAB) m/z 335 (M+H)

A-157: 2-(indan-2-yloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.36 (d, 1H, J=7.7Hz), 7.29-7.17 (m, 4H), 5.91 (m, 1H), 3.52 (dd, 2H, J=16.9, 6.9 Hz),3.14 (dd, 2H, J=16.9, 4.1 Hz); IR (neat) 2915, 2236, 1590, 1463, 1431,1348, 1267, 1188, 1148, 1008, 972, 938, 841, 744 cm⁻¹; MS (FAB) m/z 305(M+H)

A-158: 2-(4-chloro-benzyloxy)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) d 8.07 (d, 1H, J=7.7 Hz), 7.49-7.32 (m, 4H),7.37 (d, 1H, J=7.7 Hz), 5.52 (s, 2H); IR (neat) 2237, 1591, 1492, 1464,1432, 1402, 1348, 1269, 1187, 1149, 1116, 987, 843, 809, 745 cm⁻¹; MS(FAB) m/z 313 (M+H)

The compounds A-159 and A-161 were obtained from the respective alkynecompounds by using the following procedure.

Triethylamine (11 mmol) and Lindlar's catalyst (7 wt-%, 1 mmol) wereadded to a solution of the alkyne (10 mmol) in DMF (25 mL). The reactionflask was evacuated, purged with hydrogen five times, and then stirredunder a hydrogen atmosphere for 8 h. The reaction mixture was filteredover celite and washed with diethyl acetate (25 mL). The resultingsolution was washed with 2 wt-% aq. NH₄Cl soln. (37 mL) and then twicewith water (2×25 mL), dried over MgSO₄, filtered, and concentrated invacuo The residue was purified by flash column chromatography on silicagel using EA/hexanes (1:4) as eluent.

A-159: 2-but-2-enyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.34 (d, 1H, J=7.7Hz), 5.81 (m, 1H), 5.72 (m, 1H), 5.09 (d, 2H, J=6.6 Hz), 1.81 (d, 3H,J=6.8 Hz)

IR (neat) 2919, 2237, 1591, 1466, 1433, 1335, 1267, 1188, 1150, 1118,969, 842, 747 cm⁻¹; MS (FAB) m/z 243 (M+H)

A-160: 2-but-2-ynyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.08 (d, 1H, J=7.5 Hz), 7.39 (d, 1H, J=7.7Hz), 5.10 (q, 2H, J=2.4 Hz), 1.87 (t, 3H, J=2.3 Hz); IR (neat) 2924,2239, 1590, 1460, 1429, 1348, 1271, 1189, 1151, 1117, 977, 931, 844, 745cm⁻¹; MS (FAB) m/z 241 (M+H)

A-161: 2-pent-2-enyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.05 (d, 1H, J=7.7 Hz), 7.34 (d, 1H, J=7.7Hz), 5.73-5.65 (m, 2H), 5.07 (d, 2H, J=6.0 Hz), 2.23 (m, 2H), 1.03 (t,3H, J=7.6 Hz); IR (neat) 2967, 2237, 1590, 1465, 1431, 1405, 1342, 1267,1187, 1151, 1118, 976, 842, 746 cm⁻¹; MS (FAB) m/z 257 (M+H)

A-162: 2-pent-2-ynyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.08 (d, 1H, J=7.7 Hz), 7.39 (d, 1H, J=7.7Hz), 5.11 (t, 2H, J=2.1 Hz), 2.23 (m, 2H), 1.14 (t, 3H, J=7.5 Hz); IR(neat) 2982, 2238, 1590, 1461, 1428, 1348, 1272, 1189, 1151, 1117, 979,844 cm⁻¹; MS (FAB) m/z 255 (M+H)

A-163: 2-p-tolyloxy-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.17 (d, 1H, J=7.7 Hz), 7.44 (d, 1H, J=7.7 Hz), 7.22 (d, 2H, J=8.6 Hz),7.10 (m, 2H), 2.39 (s, 3H); IR (neat) 2921, 2237, 1585, 1508, 1462,1409, 1348, 1269, 1188, 1149, 1115, 947, 853 cm⁻¹; MS (FAB) m/z 279(M+H)

A-164: 2-cyclopentyloxy-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.67 (d, 1H, J=7.9 Hz), 7.23 (d, 1H, J=7.9Hz), 7.17 (bs, 1H), 4.92 (m, 1H), 1.80-2.23 (m, 6H), 1.61-1.77 (m, 2H)

IR (neat) 2959, 2232, 1506, 1435, 1328, 1245, 1163, 1122, 1079, 877, 825cm⁻¹ MS (FAB) m/z 256 (M+H)

A-165: 2-cyclohexyloxy-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.68 (d, 1H, J=8.1 Hz), 7.23 (d, 1H, J=8.0Hz), 7.17 (bs, 1H), 4.49 (m, 1H), 1.78-2.02 (m, 4H), 1.63-1.77 (m, 2H),1.35-1.62 (m, 4H); IR (neat) 2939, 2862, 2233, 1615, 1503, 1430, 1328,1247, 1176, 1132, 1075, 1018, 970, 904, 829 cm⁻¹; MS (FAB) m/z 270 (M+H)

A-166: 2-butoxy-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.68 (d, 1H, J=8.0 Hz), 7.14-7.30 (m, 2H),4.13 (t, 2H, J=6.4 Hz), 1.81-1.93 (m, 2H), 1.49-1.62 (m, 2H), 1.01 (t,3H, J=7.3 Hz); IR (neat) 2962, 2223, 1616, 1580, 1505, 1432, 1393, 1329,1251, 1176, 1133, 1075, 975, 919, 865, 829 cm⁻¹; MS (FAB) m/z 244 (M+H)

A-167: 2-cyclopentyloxy-4-methyl-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.16 (s, 1H), 5.54 (m, 1H), 2.58 (s, 3H), 2.02(m, 2H), 1.85 (m, 4H), 1.64 (m, 2H); IR (neat) 2967, 2232, 1576, 1348,1314, 1075, 913, 865 cm⁻¹; MS (FAB) m/z 271(M+H)

A-168: 2-butoxy-4-tert-butyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.40 (d, 1H, J=8.2 Hz), 7.0 (dd, 1H, J=1.6,1.6 Hz), 6.90 (d, 1H, J=1.4 Hz), 4.0 (t, 2H, J=6.4 Hz), 1.88-1.74 (m,2H), 1.61-1.50 (m, 2H), 1.3 (s, 9H), 0.9 (t, 3H, J=1.8 Hz)

IR (neat) 2963, 2224, 1604, 1412, 1237 cm⁻¹

A-169: 4-tert-butyl-2-isobutoxy-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.47 (d, 1H, J=8.2 Hz), 7.0 (dd, 1H, J=1.6,1.6 Hz), 6.92 (d, 1H, J=1.4 Hz), 3.83 (d, 2H, J=6.4 Hz), 2.24-2.10 (m,1H), 1.32 (s, 9H), 1.08 (d, 6H, J=6.8 Hz)

IR (neat) 2963, 2225, 1606, 1563, 1501, 1469 cm⁻¹

A-170: 4-tert-butyl-2-cyclohexyloxy-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.46 (d, 1H, J=8.0 Hz), 7.0 (dd, 1H, J=1.6,1.6 Hz), 6.95 (d, 1H, J=1.6 Hz), 4.43-4.39 (m, 1H), 2.0-1.77 (m, 4H),1.77-1.60 (m, 4H), 1.48-1.37 (m, 2H), 1.31 (s, 9H)

IR (neat) 2934, 2858, 2225, 1741, 1604, 1563 cm⁻¹

A-171: 4-tert-butyl-2-(2,2-dimethyl-propoxy)-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.46 (d, 1H, J=8.2 Hz), 7.0 (dd, 1H, J=1.6,1.6 Hz), 6.91 (d, 1H, J=1.4 Hz), 3.70 (s, 2H), 1.32 (s, 9H), 1.09 (s,9H)

IR (neat) 2963, 2225, 1605, 1564, 1500, 1468 cm⁻¹

A-172: 4-tert-butyl-2-cyclopentyloxy-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.45 (d, 1H, J=8.0 Hz), 6.99-6.92 (m, 2H),4.91-4.86 (m, 1H), 1.96-1.83 (m, 6H), 1.67-1.58 (m, 2H), 1.31 (s, 9H)

IR (neat) 2963, 2872, 2224, 1604, 1563, 1498 cm⁻¹

A-173: 4-tert-butyl-2-pentoxy-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.46 (d, 1H, J=8.0 Hz), 7.0 (dd, 1H, J=1.6,1.6 Hz), 6.93 (d, 1H, J=1.6 Hz), 4.07 (t, 2H, J=6.4 Hz), 1.90-1.81 (m,2H), 1.54-1.35 (m, 4H), 1.31 (s, 9H), 0.94 (t, 3H, J=6.9 Hz)

IR (neat) 2960, 2870, 2225, 1605, 1564, 1500 cm⁻¹

Stage 2: Method 1:

Compounds of the general formula VI-Ca or VI-Cb (5 mmol), in which R⁵,R¹⁴, U, T and V have the above-stated meaning and m denotes 0, 1, 2 or3, palladium on carbon (10%, 500 mg) and concentrated hydrochloric acid(3 mL) are dissolved in MeOH (30 mL) and exposed to a hydrogenatmosphere for 6 hours at RT. The reaction mixture is filtered throughcelite and the filtrate is evaporated under a vacuum. The residue ispurified by means of flash chromatography (SiO₂, EA).

The following compounds B-85 to B-88 were obtained according to theabove-stated general method:

B-85: 2-cyclopentylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.68 (d, 1H, J=7.5 Hz), 7.23 (d, 1H, J=7.3 Hz), 4.95(bs, NH3), 4.30 (d, 2H), 2.39 (m, 1H), 1.96 (s, 3H, AcO—), 1.88-1.75 (m,2H), 1.68-1.54 (m, 4H), 1.42-1.30 (m, 2H); IR (neat) 2955, 2637, 2244,1539, 1426, 1369, 1141, 997 cm⁻¹

B-86: 2-ethoxy-6-trifluoromethyl-pyridin-3-ylmethyl-ammonium acetate

¹H NMR (CDCl₃) δ 7.66 (d, 1H, J=7.4 Hz), 7.23 (d, 1H, J=7.4 Hz), 5.66(bs, NH3), 4.48 (q, 2H, J=7.1 Hz), 3.91 (s, 2H), 2.00 (s, 3H, AcO), 1.42(t, 3H, J=7.0 Hz); IR (neat) 2990, 1537, 1426, 1347, 1186, 1146, 1025cm⁻¹

B-87:2-(4-ethyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.62 (d, 1H, J=7.3 Hz), 7.19 (d, 1H, J=7.5 Hz), 5.45(bs, NH3), 5.08 (m, 1H), 3.86 (s, 2H), 2.22-2.15 (m, 2H), 2.03 (s, 3H,AcO), 1.87-1.82 (m, 2H), 1.50-1.03 (m, 7H), 0.91 (t, 3H, J=6.8 Hz); IR(neat) 2926, 1572, 1421, 1355, 1275, 1186, 1141, 1010 cm⁻¹

B-88:2-(4-tert-butyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl-ammoniumacetate

¹H NMR (CDCl₃) δ 7.62 (d, 1H, J=7.1 Hz), 7.19 (d, 1H, J=7.5 Hz), 5.04(m, 1H), 4.13 (bs, NH3), 3.85 (s, 2H), 7.25-7.18 (m, 2H), 2.05 (s, 3H,AcO), 1.87-1.83 (m, 2H), 1.46-1.02 (m, 5H), 0.89 (s, 9H); IR (neat)2951, 1545, 1468, 1424, 1357, 1272, 1183 cm⁻¹

Method 2:

Compounds of the general formula VI-Ca or VI-Cb (2 mmol), in which R⁵,R¹⁴, U, T and V have the above-stated meaning and m denotes 0, 1, 2 or3, are dissolved in THF (10 mL) and BH₃.S(CH₃)_(2 [)2.0 M in THF, 3 mL,3 equivalents] is added. The reaction mixture is heated to reflux for 8hours, aq. HCl (2 N) is added and the reaction mixture is again heatedto reflux for 30 minutes. Aq. NaOH soln. and EA are added. The combinedorganic extracts are washed with sat. aq. NaCl soln. and dried overMgSO₄. The solvent is evaporated under a vacuum and the residue ispurified by flash chromatography (SiO₂, different mixtures of methylenechloride and methanol).

The following compounds B-89 to B-144 were obtained according to theabove-stated general method:

B-89: C-[2-(3-methyl-butoxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.63 (d, 1H, J=7.8 Hz), 7.21 (d, 1H, J=7.8 Hz), 4.43 (t, 1H, J=6.9 Hz),3.84 (s, 2H), 2.43 (bs, 2H), 1.60-1.89 (m, 3H), 0.97 (d, 6H, J=6.6 Hz);MS (FAB) m/z 263 (M+H)

B-90:C-[2-(3,3-dimethyl-butoxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.56 (d, 1H, J=7.8 Hz), 7.13 (d, 1H, J=7.8 Hz), 4.38 (t, 1H, J=6.9 Hz),3.74 (s, 2H), 1.64 (t, 2H, J=6.9 Hz), 0.92 (s, 9H); MS (FAB) m/z 277(M+H)

B-91:C-[2-(2-methyl-cyclopropylmethoxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.63 (d, 1H, J=7.8 Hz), 7.21 (d, 1H, J=7.8Hz), 4.24 (m, 2H), 3.85 (s, 2H), 1.08 (d, 3H, J=6.0 Hz), 0.98 (m, 1H),0.77 (m, 1H), 0.52 (m, 1H), 0.34 (m, 1H); MS (FAB) m/z 261 (M+H)

B-92: C-[2-butoxy-6-(chloro-difluoro-methyl)-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.71 (d, 1H, J=7.8 Hz), 6.98 (d, 1H, J=7.8 Hz), 3.99 (s, 2H), 3.59 (t,2H, J=7.2 Hz), 1.63 (m, 2H), 1.38 (m, 2H), 0.95 (t, 3H, J=6.9 Hz); IR(neat) 2960, 1599, 1422, 1353, 1264, 1094 cm⁻¹; MS (FAB) m/z 265(M+H)

B-93: C-(2-phenoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.86 (dd, 1H, J=7.5, 1.5 Hz), 7.35-7.43 (m, 3H, 7.15-7.23 (m, 3H), 4.03(s, 2H); IR (neat) 2922, 1589, 1490, 1468, 1405, 1257, 1186, 1138, 941,839, 752, 691 cm⁻¹; MS (FAB) m/z 269(M+H)

B-94: C-(2-butoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.65 (d, 1H, J=7.3 Hz), 7.21 (d, 1H, J=7.3 Hz), 4.41(t, 2H, J=6.4 Hz), 3.84 (s, 2H), 1.78 (m, 2H), 1.50 (m, 2H), 0.98 (t,3H, J=7.3 Hz); IR (neat) 2963, 1607, 1470, 1425, 1357, 1193, 1132 cm⁻¹

B-95: C-(2-isopropoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.63 (d, 1H, J=7.3 Hz), 7.19 (d, 1H, J=7.3 Hz), 5.42(m, 1H), 3.82 (s, 2H), 1.37 (d, 6H, J=6.2 Hz); IR(neat) 3370, 2983,1602, 1467, 1421, 1341, 1268, 1178, 1141, 969 cm⁻¹

B-96: C-(2-cyclopentyloxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.62 (d, 1H, J=7.3 Hz), 7.19 (d, 1H, J=7.3 Hz), 5.53(m, 1H), 3.81 (s, 2H), 2.05-1.95 (m, 2H), 1.82-1.63 (m, 6H)

B-97: C-(2-cyclohexyloxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.63 (d, 1H, J=7.3 Hz), 7.18 (d, 1H, J=7.5 Hz), 5.20(m, 1H), 3.83 (s, 2H), 1.99-1.95 (m, 2H), 1.78-1.39 (m, 8H); IR (neat)2937, 2860, 1603, 1462, 1421, 1362, 1264, 1140, 972 cm⁻¹

B-98: C-(2-hexyloxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.65 (d, 1H J=7.3 Hz), 7.22 (d, 1H, J=7.3 Hz), 4.40 (t,2H, J=6.6 Hz), 3.85 (s, 2H), 1.84-1.74 (m, 2H), 1.50-1.30 (m, 6H), 0.90(t, 3H, J=7.0 Hz); IR (neat) 2929, 1603, 1465, 1424, 1361, 1266, 1179,1141 cm⁻¹

B-99: C-(2-isobutoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.66 (d, 1H, J=7.3 Hz), 7.22 (d, 1H, J=7.3 Hz), 4.18(d, 2H, J=6.6 Hz), 3.86 (s, 2H), 2.12 (m, 1H), 1.04 (d, 6H, J=6.8 Hz)

IR (neat) 2964, 1603, 1465, 1424, 1362, 1266, 1178, 1140, 1011 cm⁻¹

B-100:C-(2-cyclopropylmethoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.65 (d, 1H, J=7.5 Hz), 7.21 (d, 1H, J=7.3 Hz), 4.25(d, 2H, J=7.1 Hz), 3.87 (s, 2H), 1.34-1.25 (m, 1H), 0.63-0.57 (m, 2H),0.39-0.35 (m, 2H); IR (neat) 2948, 1603, 1465, 1427, 1388, 1263, 1177,1138, 990 cm⁻¹

B-101:C-(2-cyclobutylmethoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.64 (d, 1H, J=6.6 Hz), 7.22 (d, 1H, J=7.5 Hz), 4.37(d, 2H, J=6.8 Hz), 3.85 (s, 2H), 2.85-2.75 (m, 1H), 2.17-1.85 (m, 6H);IR (neat) 2933, 1602, 1464, 1422, 1365, 1265, 1178, 1140, 998 cm⁻¹

B-102: 2-butoxy-4-trifluoromethyl-benzylamine

¹H NMR (CDCl₃) δ 7.33 (d, 1H, J=7.9 Hz), 7.18 (d, 1H, J=7.7 Hz), 7.05(s, 1H), 4.04 (t, 2H, J=6.4 Hz), 3.87 (s, 2H), 1.83 (m, 2H), 1.51 (m,2H), 1.00 (t, 3H, J=7.3 Hz); IR (neat) 3340, 2953, 1617, 1507, 1428,1336, 1243, 1119 cm⁻¹

B-103: C-(2-propoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.65 (dd, 1H, J=7.3, 0.8 Hz), 7.22 (d, 1H, J=7.3 Hz),4.37 (t, 2H, J=6.6 Hz), 3.85 (s, 2H), 1.88-1.77 (m, 2H), 1.04 (t, 3H,J=7.5 Hz); IR (neat) 2970, 1603, 1466, 1425, 1364, 1268, 1178, 1140 cm⁻¹

B-104: C-(2-pentyloxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.65 (d, 1H, J=7.3 Hz), 7.22 (d, 1H, J=7.3 Hz), 4.40(t, 2H, J=6.6 Hz), 3.85 (s, 2H), 1.91-1.67 (m, 2H), 1.46-1.35 (m, 4H),0.93 (t, 3H, J=7.3 Hz); IR (neat) 2957, 1465, 1424, 1361, 1267, 1179,1140 cm⁻¹

B-105: C-(2-cyclobutoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.64 (d, 1H, J=7.5 Hz), 7.20 (d, 1H, J=7.4 Hz), 5.28(m, 1H), 3.85 (s, 2H), 2.53-2.47 (m, 2H), 2.15-2.10 (m, 2H), 1.88-1.69(m, 2H); IR (neat) 2990, 1602, 1466, 1420, 1346, 1265, 1178, 1139, 959cm⁻¹

B-106:C-[2-(4-methyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (CDCl₃) δ 7.62 (d, 1H, J=7.4 Hz), 7.18 (d, 1H, J=T4 Hz), 5.07 (m,1H), 3.81 (s, 2H), 2.18-2.15 (m, 2H), 1.79-1.76 (m, 2H), 1.51-1.39 (m,3H), 1.17-1.08 (m, 2H), 0.93 (d, 3H, J=6.5 Hz); IR (neat) 2929, 1603,1462, 1420, 1356, 1266, 1178, 1140, 1005 cm⁻¹

B-107: C-(6-tert-butyl-2-cyclohexyloxy-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.37 (d, 1H, J=7.5 Hz), 6.77 (d, 1H, J=7.5 Hz), 5.15(m, 1H), 3.76 (bs, NH2), 3.48 (s, 2H), 2.30-1.39 (m, 10H), 1.30 (s, 9H);

IR (neat) 2935, 1582, 1452, 1406, 1363, 1254, 982 cm⁻¹

B-108: C-(6-tert-butyl-2-cyclopentyloxy-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.36 (d, 1H, J=7.4 Hz), 6.78 (d, 1H, J=7.3 Hz), 5.50(m, 1H), 3.73 (s, 2H), 2.11 (bs, NH2), 2.03-1.63 (m, 8H), 1.31 (s, 9H);IR (neat) 2960, 1583, 1454, 1406, 1350, 1255, 988 cm⁻¹

B-109: C-(2-butoxy-6-tert-butyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.38 (d, 1H, J=7.5 Hz), 6.80 (d, 1H, J=7.5 Hz), 4.39(t, 2H, J=6.6 Hz), 3.77 (s, 2H), 2.17 (bs, NH2), 1.77 (m, 2H), 1.49 (m,2H), 1.31 (s, 9H), 0.98 (t, 3H, J=7.4 Hz); IR (neat) 2958, 1583, 1458,1411, 1364, 1254 cm⁻¹

B-110: C-(6-tert-butyl-2-hexyloxy-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.37 (d, 1H, J=7.3 Hz), 6.79 (d, 1H, J=7.5 Hz), 4.37(t, 2H, J=6.6 Hz), 3.74 (s, 2H), 1.78 (m, 2H), 1.48-1.30 (m, 6H), 1.31(s, 9H), 0.90 (m, 3H); IR (neat) 2956, 1582, 1458, 1411, 1361, 1253,1016 cm⁻¹

B-111: C-(2-benzyloxy-6-tert-butyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.47-7.29 (m, 6H), 6.83 (d, 1H, J=7.5 Hz), 5.47 (s,2H), 3.79 (s, 2H), 1.31 (s, 9H); IR (neat) 2957, 1582, 1454, 1405, 1357,1253, 1009 cm⁻¹

B-112:C-(2-cyclohexylmethoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.64 (d, 1H, J=7.3 Hz), 7.21 (d, 1H, J=7.3 Hz), 4.20(d, 2H), 3.85 (s, 2H), 1.86-1.67 (m, 5H), 1.32-1.00 (m, 6H)

B-113:C-[2-(4-methyl-cyclohexylmethoxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (CDCl₃) δ 7.78 & 7.64 (d, 1H), 7.21 (d, 1H, J=7.3 Hz), 4.40 &3.85 (s, 2H), 4.31 & 4.20 (m, 2H), 2.00-1.50 (m, 7H), 1.40-1.00 (m, 3H),0.95-0.87 (m, 3H); IR (neat) 2923, 1602, 1462, 1423, 1359, 1264, 1177,1140, 1110 cm⁻¹

B-114:C-[2-(2,2-dimethyl-cyclopropylmethoxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (CDCl₃) δ 7.64 (d, 1H, J=7.3 Hz), 7.21 (d, 1H, J=7.3 Hz), 4.63(dd, 1H, J=11.5, 6.6 Hz), 4.20 (dd, 1H, J=11.6, 8.9 Hz), 3.86 (s, 2H),1.14 (s, 3H), 1.10 (s, 3H), 0.88 (m, 1H), 0.58 (dd, 1H, J=8.6, 4.4 Hz),0.30 (dd, 1H, J=4.8, 4.8 Hz); IR (neat) 2951, 1603, 1464, 1426, 1396,1344, 1264, 1178, 1141, 987 cm⁻¹

B-115:4-(3-aminomethyl-6-trifluoromethyl-pyridin-2-yloxymethyl)-piperidine-1-carbonicacid tert-butyl ester

¹H NMR (CDCl₃) δ 7.69 (d, 1H, J=7.5 Hz), 7.24 (d, 1H, J=7.5 Hz), 4.27(d, 2H), 4.20-4.07 (m, 2H), 3.86 (s, 2H), 2.80-2.65 (m, 2H), 1.83-1.50(m, 3H), 1.47 (s, 9H), 1.35-1.20 (m, 2H); IR (neat) 3392, 2926, 1688,1424, 1361, 1268, 1174, 1142, 1017 cm⁻¹

B-116:C-[6-trifluoromethyl-2-(4-trifluoromethyl-cyclohexyloxy)-pyridin-3-yl]-methylamine

IR (neat) 2923, 1603, 1465, 1424, 1363, 1269, 1180, 1139 cm⁻¹

B-117:4-(3-aminomethyl-6-trifluoromethyl-pyridin-2-yloxy)-piperidine-1-carbonicacid tert-butyl ester

¹H NMR (CDCl₃) δ 7.69 (d, 1H, J=6.8 Hz), 7.24 (d, 1H, J=7.3 Hz), 5.36(m, 1H), 3.85 (s, 2H), 3.68 (m, 2H), 3.40 (m, 2H), 2.05-1.60 (m, 4H),1.48 (s, 9H)

IR (neat) 3393, 2928, 1688, 1421, 1363, 1272, 1237, 1173, 1139, 1028cm⁻¹

B-118:C-[2-(pyridin-4-ylmethoxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.62 (d, 2H, J=6.0 Hz), 7.78 (d, 1H, J=7.2 Hz), 7.38 (d, 2H, J=6.2 Hz),7.31 (d, 1H, J=7.6 Hz), 5.49 (s, 2H), 3.96 (s, 2H)

IR (neat) 3367, 1602, 1468, 1417, 1359, 1267, 1179, 1137, 1179, 1137,1024, 936, 840, 801 cm⁻¹; MS (FAB) m/z 284 (M+H)

B-119: C-(2-phenethyloxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.63 (d, 1H, J=7.2 Hz), 7.38-7.21 (m, 6H), 4.63 (t, 2H, J=6.6 Hz), 3.78(s, 2H), 3.11 (t, 2H, J=6.6 Hz), 1.61 (bs, 2H)

IR (neat) 3029, 2956, 1599, 1463, 1423, 1354, 1270, 1180, 1139, 1004,951, 839, 747, 701 cm⁻¹; MS (FAB) m/z 297 (M+H)

B-120:C-[2-(pyridin-2-ylmethoxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.61 (d, 1H, J=4.9 Hz), 7.75 (d, 1H, J=7.7 Hz), 7.71 (td, 1H, J=7.7, 1.7Hz), 7.48 (d, 1H, J=7.9 Hz), 7.26 (m, 2H), 5.61 (s, 2H), 3.98 (s, 2H),2.13 (bs, 2H); IR (neat) 3395, 2920, 1598, 1417, 1355, 1274, 1181, 1137,1002, 936, 840, 756 cm⁻¹; MS (FAB) m/z 284 (M+H)

B-121: C-(2-benzyloxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.70 (d, 1H, J=7.3 Hz), 7.48 (m, 2H), 7.42-7.35 (m, 4H), 5.47 (s, 2H),3.70 (s, 2H), 1.76 (bs, 2H); IR (neat) 2925, 1652, 1600, 1539, 1459,1419, 1355, 1267, 1179, 1138, 992, 838, 741, 698 cm⁻¹; MS (FAB) m/z 283(M+H)

B-122: 2-benzyloxy-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.51-7.35 (m, 6H), 7.22 (d, 1H, J=7.7 Hz), 7.16 (s, 1H), 5.13 (s, 2H),3.92 (s, 2H), 1.60 (bs, 2H); IR (neat) 2920, 1509, 1426, 1328, 1239,1166, 1122, 1019, 917, 858, 740, 697 cm⁻¹; MS (FAB) m/z 282 (M+H)

B-123:C-[2-(pyridin-3-ylmethoxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.75 (s, 1H), 8.58 (d, 1H, J=4.4 Hz), 7.84 (d, 1H, J=7.7 Hz), 7.74 (d,1H, J=7.5 Hz), 7.31 (d, 1H, J=4.9 Hz), 7.29 (d, 1H, J=7.3 Hz), 5.50 (s,2H), 3.89 (s, 2H), 1.68 (bs, 2H); IR (neat) 2920, 1599, 1538, 1462,1416, 1356, 1267, 1179, 1137, 997, 840 cm⁻¹; MS (FAB) m/z 284 (M+H)

B-124:C[6-trifluoromethyl-2-(4-trifluoromethyl-benzyloxy)-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.74 (d, 1H, J=7.3 Hz), 7.69-7.54 (m, 4H), 7.29 (d, 1H, J=7.5 Hz), 5.53(s, 2H), 3.91 (s, 2H), 1.50 (bs, 2H); IR (neat) 2919, 1600, 1467, 1419,1356, 1326, 1267, 1131, 1067, 1014, 936, 826 cm⁻¹; MS (FAB) m/z 351(M+H)

B-125:C-[2-(4-butyl-benzyloxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.68 (d, 1H, J=7.5 Hz), 7.39 (d, 2H, J=7.9 Hz), 7.25 (d, 1H, J=7.4 Hz),7.19 (d, 2H, J=8.0 Hz), 5.43 (s, 2H), 3.87 (s, 2H), 2.61 (t, 2H, J=7.9Hz), 1.60 (m, 2H), 1.36 (m, 2H), 0.93 (t, 3H, J=7.3 Hz)

IR (neat) 2929, 1599, 1463, 1420, 1353, 1267, 1180, 1141, 990, 836 cm⁻¹;MS (FAB) m/z 339 (M+H)

B-126:C-[2-(4-tert-butyl-benzyloxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.68 (d, 1H, J=7.3 Hz), 7.49-7.34 (m, 4H), 7.25 (d, 1H, J=7.5 Hz), 5.44(s, 2H), 3.87 (s, 2H), 1.52 (bs, 2H), 1.33 (s, 9H)

IR (neat) 2963, 1599, 1516, 1464, 1421, 1354, 1267, 1179, 1140, 990, 837cm⁻¹; MS (FAB) m/z 339 (M+H)

B-127: C-[2-(indan-2-yloxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.66 (d, 1H, J=8.1 Hz), 7.25 (d, 1H, J=8.0 Hz), 7.24-7.15 (m, 4H), 5.91(m, 1H), 3.76 (s, 2H), 3.48 (dd, 2H, J=17.0, 6.6 Hz), 3.14 (dd, 2H,J=16.9, 3.7 Hz), 1.43 (bs, 2H); IR (neat) 2953, 1676, 1596, 1464, 1418,1348, 1266, 1186, 1139, 1012, 970, 935, 843, 743 cm⁻¹; MS (FAB) m/z 309(M+H)

B-128:C-[2-(4-chloro-benzyloxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.71 (d, 1H, J=7.3 Hz), 7.44-7.32 (m, 4H), 7.27 (d, 1H, J=7.3 Hz), 5.43(s, 2H), 3.88 (s, 2H), 1.50 (bs, 2H); IR (neat) 2919, 1600, 1493, 1465,1423, 1355, 1264, 1179, 1138, 1110, 997, 935, 839 cm⁻¹; MS (FAB) m/z 317(M+H)

B-129:C-[6-(chloro-difluoro-methyl)-2-cyclopentyloxy-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.60 (d, 1H, J=7.3 Hz), 7.16 (d, 1H, J=7.5 Hz), 5.52 (m, 1H), 3.81 (m,2H), 1.95-2.10 (m, 2H), 1.60-1.90 (m, 6H); IR (neat) 3367, 2961, 1599,1456, 1418, 1349, 1265, 1096, 991, 888, 827 cm⁻¹; MS (FAB) m/z 277 (M+H)

B-130:C-[6-(chloro-difluoro-methyl)-2-cyclohexyloxy-pyridin-3-yl]-methylamine

¹H NMR (400 MHz, CDCl₃)

117.61 (d, 1H, J=7.6 Hz), 7.15 (d, 1H, J=7.6 Hz), 5.19 (m, 1H), 3.83 (s,2H), 1.93-2.04 (m, 2H), 1.70-1.82 (m, 2H), 1.52-1.66 (m, 6H); IR (neat)2936, 2858, 1600, 1455, 1419, 1364, 1263, 1096, 989, 881 cm⁻¹; MS (FAB)m/z 291 (M+H)

B-131:C-[6-(chloro-difluoro-methyl)-2-(pyridin-3-ylmethoxy)-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 8.76 (s, 1H), 8.57 (m, 1H), 7.85 (m, 1H), 7.72(d, 1H, J=7.1 Hz), 7.31 (m, 1H), 7.25 (d, 1H, J=7.5 Hz), 5.51 (bs, 2H),3.88 (s, 2H); IR (neat) 2922, 1598, 1456, 1414, 1357, 1096, 1005, 884,829, 712 cm⁻¹; MS (FAB) m/z 300 (M+H)

B-132:C-[6-(chloro-difluoro-methyl)-2-(pyridin-2-ylmethoxy)-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 8.59 (m, 1H), 7.68-7.84 (m, 2H), 7.47 (m, 1H),7.21-7.26 (m, 2H), 5.66 (s, 2H), 4.09 (s, 2H); IR (neat) 2921, 1597,1416, 1350, 1272, 1097, 1011, 969, 832, 763 cm⁻¹; MS (FAB) m/z 300 (M+H)

B-133:C-[6-(chloro-difluoro-methyl)-2-isobutoxy-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.63 (d, 1H, J=7.4 Hz), 7.19 (d, 1H, J=7.5 Hz), 4.15-4.23 (m, 2H), 3.86(bs, 2H), 2.12 (m, 1H), 1.04 (d, 6H, J=6.7 Hz); IR (neat) 2963, 1599,1460, 1422, 1361, 1264, 1184, 1095, 1012, 970, 880, 826 cm⁻¹; MS (FAB)m/z 265 (M+H)

B-134: 2-cyclopentyloxy-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.32 (d, 1H, J=7.5 Hz), 7.15 (d, 1H, J=7.7 Hz), 7.04 (bs, 1H), 4.86 (m,1H), 3.82 (s, 2H), 1.60-2.02 (m, 8H); IR (neat) 2962, 1590, 1507, 1427,1331, 1238, 1167, 1122, 989, 916, 862 cm⁻¹; MS (FAB) m/z 260 (M+H)

B-135: 2-cyclohexyloxy-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.34 (d, 1H, J=7.9 Hz), 7.15 (d, 1H, J=7.7 Hz), 7.05 (bs, 1H), 4.39 (m,1H), 3.86 (s, 2H), 1.90-2.00 (m, 4H), 1.70-1.89 (m, 2H), 1.51-1.69 (m,2H), 1.32-1.51 (m, 2H); IR (neat) 2938, 2860, 1589, 1507, 1426, 1329,1234, 1164, 1122, 1078, 1044, 973, 906, 862 cm⁻¹; MS (FAB) m/z 274 (M+H)

B-136: 2-butoxy-4-trifluoromethyl-benzylamine

¹H NMR (300 MHz, CDCl₃)

7.34 (d, 1H, J=7.7 Hz), 7.18 (d, 1H, J=7.7 Hz), 7.05 (bs, 1H), 4.04 (t,2H, J=6.2 Hz), 3.87 (s, 2H), 1.72-1.85 (m, 2H), 1.41-1.60 (m, 2H), 1.00(t, 3H, J=7.3 Hz); IR (neat) 3304, 2957, 1507, 1427, 1382, 1330, 1239,1159, 1114, 919, 861, 822 cm⁻¹; MS (FAB) m/z 248 (M+H)

B-137:C-(2-cyclopentyloxy-4-methyl-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.04 (s, 1H), 5.51 (m, 1H), 3.82 (s, 2H), 2.38(s, 3H), 2.01 (m, 2H), 1.75 (m, 6H); IR (neat) 2964, 1574, 1288, 1061,993, 917, 865, 723 cm⁻¹; MS (FAB) m/z 275(M+H)

B-138:C-[2-(1-butyl-pentyloxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.62 (d, 1H, J=7.3 Hz), 7.18 (d, 1H, J=7.5Hz), 5.32 (m, 1H), 3.82 (s, 2H), 1.67-1.75 (m, 2H), 1.33 (m, 9H), 0.90(m, 7H); IR (neat) 2932, 2865, 1601, 1464, 975, 835, 744, 701 cm⁻¹; MS(FAB) m/z 319(M+H)

B-139: C-(2-p-tolyloxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃)

7.84 (d, 1H, J=7.3 Hz), 7.35 (d, 1H, J=7.5 Hz), 7.19 (d, 2H, J=8.8 Hz),7.06 (m, 2H), 4.02 (s, 2H), 2.37 (s, 3H); IR (neat) 2923, 1596, 1511,1463, 1403, 1262, 1142, 943, 816 cm⁻¹; MS (FAB) m/z 283 (M+H)

B-140:C-(4-methyl-2-pentyloxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.06 (s, 1H), 4.37 (t, 2H, J=6.6 Hz), 3.85 (s,2H), 2.40 (s, 3H), 1.80 (m, 2H), 1.45 (m, 2H), 1.39-1.31 (m, 4H), 0.90(m, 3H)

IR (neat) 2931, 1610, 1575, 1463, 1409, 1348, 1290, 1246, 1177, 1138,1073, 917, 866, 721 cm⁻¹; MS (FAB) m/z 277 (M+H)

B-141: C-(2-methoxy-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (CDCl₃) δ 7.67 (d, 1H, J=7.3 Hz), 7.25 (d, 1H), 4.03 (s, 3H),3.85 (s, 2H);

IR (neat) 3400, 2923, 1738, 1468, 1370, 1268, 1137 cm⁻¹

B-142:C-[2-(4-ethyl-benzyloxy)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.68 (d, 1H, J=7.3 Hz), 7.41 (d, 2H, J=7.9 Hz), 7.25 (d, 1H, J=7.2 Hz),7.21 (d, 2H, J=7.9 Hz), 5.44 (s, 2H), 3.87 (s, 2H), 2.66 (q, 2H, J=7.5Hz), 1.63 (bs, 2H), 1.24 (t, 3H, J=7.6 Hz); IR (neat) 2965, 1600, 1463,1419, 1354, 1265, 1178, 1138, 1111, 990, 825 cm⁻¹; MS (FAB) m/z 311(M+H)

B-143:C-[2-benzyloxy-6-(chloro-difluoro-methyl)-pyridin-3-yl]-methylamine

¹H NMR (400 MHz, CDCl₃)

7.67 (d, 1H, J=7.6 Hz), 7.45-7.52 (m, 2H), 7.28-7.40 (m, 3H), 7.22 (d,1H, J=7.6 Hz), 5.48 (s, 2H), 3.88 (s, 2H); IR (neat) 2923, 1599, 1456,1416, 1356, 1256, 1096, 1000, 883, 872, 698 cm⁻¹; MS (FAB) m/z 299 (M+H)

B-144:C-[6-(chloro-difluoro-methyl)-2-hexyloxy-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

7.62 (d, 1H, J=7.3 Hz), 7.18 (d, 1H, J=7.5 Hz), 4.34-4.44 (m, 2H),3.80-3.85 (m, 2H), 1.70-1.84 (m, 2H), 1.21-1.52 (m, 6H), 0.85-0.95 (m,3H); IR (neat) 2930, 1600, 1460, 1423, 1364, 1264, 1096, 1002, 879, 827cm⁻¹; MS (FAB) m/z 293 (M+H)

Method 3:

Compounds of the general formula VI-Ca or VI-Cb (1.5 mmol), in which R⁵,R¹⁴, U, T and V have the above-stated meaning and m denotes 0, 1, 2 or3, are dissolved in diethylether (3 mL) and a suspension of lithiumaluminium hydride (3 mmol) in diethylether (5 mL) is slowly added. Thereaction mixture is heated to reflux for 4 hours, and methanol and 1 Naq. NaOH soln. are slowly added at 0° C. The reaction mixture is dilutedwith methanol and filtered over celite. The solvent is evaporated undera vacuum and the residue is purified by flash chromatography (SiO₂,different mixtures of methylene chloride and methanol).

The following compounds B-145 to B-150 were obtained according to theabove-stated general method:

B-145: 2-butoxy-4-tert-butyl-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.17 (d, 1H, J=7.8 Hz), 6.92 (dd, 1H, J=1.6,1.6 Hz), 6.88 (d, 1H, J=1.6 Hz), 4.02 (t, 2H, J=6.4 Hz), 3.85 (bs, 2H),1.85-1.76 (m, 2H), 1.57-1.44 (m, 2H), 1.3 (s, 9H), 0.98 (t, 3H, J=7.3Hz)

IR (neat) 2959, 2869, 1612, 1576, 1507, 1468 cm⁻¹

B-146: 4-tert-butyl-2-isobutoxy-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.18 (d, 1H, J=7.7 Hz), 6.92 (dd, 1H, J=1.6,1.6 Hz), 6.86 (d, 1H, J=1.6 Hz), 4.15 (bs, 2H), 3.80 (s, 2H), 3.78 (d,2H, J=6.4 Hz), 2.18-2.10 (m, 1H), 1.30 (s, 9H), 1.05 (d, 6H, J=6.6 Hz)

IR (neat) 2958, 1614, 1513, 1409, 1269, 1232 cm⁻¹

B-147: 4-tert-butyl-2-cyclohexyloxy-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.18 (d, 1H, J=7.5 Hz), 6.91-6.89 (m, 2H),5.29 (bs, 2H), 4.43-4.30 (m, 1H), 3.88 (s, 2H), 2.03-1.25 (m, 10H), 1.29(s, 9H)

IR (neat) 2932, 2875, 1611, 1504, 1455, 1412 cm⁻¹

B-148: 4-tert-butyl-2-(2,2-dimethyl-propoxy)-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.22 (d, 1H, J=7.8 Hz), 6.94 (dd, 1H, J=1.6,1.6 Hz), 6.86 (s, 1H), 5.41 (bs, 2H), 3.95 (s, 2H), 3.60 (s, 2H), 1.30(s, 9H), 1.06 (s, 9H)

IR (neat) 2958, 2867, 1613, 1577, 1475, 1410 cm⁻¹

B-149: 4-tert-butyl-2-cyclopentyloxy-benzyl amine

¹H NMR (300 MHz, CDCl₃) δ 7.12 (d, 1H, J=8.2 Hz), 6.90-6.88 (m, 2H),4.86-4.80 (m, 1H), 3.75 (s, 2H), 2.94 (bs, 2H), 1.95-1.61 (m, 8H), 1.30(s, 9H)

IR (neat) 2959, 1611, 1576, 1503, 1412, 1269 cm⁻¹

B-150: 4-tert-butyl-2-pentyloxy-benzylamine

¹H NMR (300 MHz, CDCl₃) δ 7.18 (d, 1H, J=7.8 Hz), 6.94-6.87 (m, 2H),4.73 (bs, 2H), 4.01 (t, 2H, J=6.4 Hz), 3.88 (s, 2H), 1.86-1.78 (m, 2H),1.51-1.35 (m, 4H), 1.30 (s, 9H), 0.93 (t, 3H, J=6.9 Hz)

IR (neat) 2958, 2866, 1614, 1511, 1463, 1415 cm⁻¹

4. General Procedure for the Preparation of Amines of General FormulaV-C

Amines of the general formula V-C are prepared as shown in scheme 3below.

Stage 1: Preparation of Nitriles of General Formula VI-D

Compounds of general formula VI-A (1 equivalent), wherein R⁵, U, T and Vhave the above-stated meaning and m denotes 0, 1, 2 or 3, are treatedwith bis(triphenylphosphine)palladium dichloride (7 mol-%) andcopper(I)iodide (14 mol-%) in 1-methyl-2-pyrrolidinon (7 mL. per mmol ofcompound of general formula VI-A). After 10 min the alkyne of generalformula HCEC-R⁸ (3.5 equivalents) and N,N-diisopropylethylamine (2equivalents) are added and the reaction mixture is stirred at atemperature between 90 and 110° C. for 12 hours. The reaction mixture isfiltered over celite and repeatedly extracted with EA. The combinedorganic phases are washed with sat. aq. NaCl soln., dried over MgSO₄ andthe solvent is removed under a vacuum. The residue is purified by flashchromatography (SiO₂, different mixtures of hexanes and EA).

The following compounds A-174 to A-180 were obtained according to theabove-stated general method:

A-174: 2-pent-1-ynyl-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.13 (d, 1H, J=8.3 Hz), 7.68 (d, 1H, 8.3 Hz), 2.55 (t, 2H, J=7.1 Hz),1.68-1.80 (m, 2H), 1.11 (t, 3H, J=7.3 Hz); IR (neat) 9969, 2230, 1569,1406, 1341, 1197, 1153, 1086, 851 cm⁻¹; MS (FAB) m/z 239 (M+H)

A-175: 2-(3,3-dimethyl-but-1-ynyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.11 (d, 1H, J=8.3 Hz), 7.66 (d, 1H, J=8.3Hz), 1.41 (bs, 9H); IR (neat) 2975, 2240, 2216, 1568, 1450, 1403, 1342,1277, 1191, 1153, 1121, 1085, 850 cm⁻¹; MS (FAB) m/z 253 (M+H)

A-176: 2-p-tolylethynyl-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.17 (d, 1H, J=8.1 Hz), 7.69 (d, 1H, J=8.1Hz), 7.57-7.65 (m, 2H), 7.24-7.26 (m, 2H), 2.41 (s, 3H); IR (neat) 3079,2216, 1567, 1413, 1343, 1286, 1184, 1143, 1112, 851, 819 cm⁻¹; MS (FAB)m/z 287 (M+H)

A-177: 2-hex-1-ynyl-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.12 (d, 1H, J=7.7 Hz), 7.67 (d, 1H, J=8.1Hz), 2.57 (d, 2H, J=7.0 Hz), 1.61-1.76 (m, 2H), 1.47-1.61 (m, 2H), 0.97(t, 3H, J=7.3 Hz); IR (neat) 2962, 2234, 1570, 1449, 1406, 1342, 1198,1153, 1124, 1085, 849, 742 cm⁻¹; MS (FAB) m/z 253 (M+H)

A-178: 2-(4-methyl-pent-1-ynyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.13 (d, 1H, J=8.1 Hz), 7.68 (d, 1H, J=8.1 Hz), 2.47 (d, 2H, J=6.4 Hz),2.04 (m, 1H), 1.11 (d, 6H, J=6.6 Hz); IR (neat) 2964, 2233, 1571, 1450,1405, 1341, 1198, 1153, 1086, 1017, 850, 743 cm⁻¹; MS (FAB) m/z 253(M+H)

A-179: 2-(3-cyclohexyl-prop-1-ynyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.12 (d, 1H, J=8.2 Hz), 7.66 (d, 1H, J=8.1Hz), 2.47 (d, 2H, J=6.6 Hz), 1.39-1.94 (m, 5H), 0.88-1.40 (m, 6H); IR(neat) 2925, 2852, 2231, 1569, 1448, 1405, 1341, 1194, 1154, 1124, 1085,847 cm⁻¹ MS (FAB) m/z 293 (M+H)

A-180: 2-(4-fluoro-phenylethynyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.19 (d, 1H, J=8.0 Hz), 7.67-7.70 (m, 3H),7.06-7.18 (m, 2H); IR (neat) 3077, 2233, 1562, 1507, 1445, 1409, 1341,1288, 1233, 1157, 1111, 840 cm⁻¹; MS (FAB) m/z 291 (M+H)

5. General Procedure for the Preparation of Amines of General FormulaV-D

Amines of the general formula V-D are prepared as shown in scheme 4below.

Stage 1: Preparation of Nitriles of General Formula VI-E

Compounds of general formula VI-A (1 equivalent), wherein R⁵, U, T and Vhave the above-stated meaning and m denotes 0, 1, 2 or 3, are treatedwith palladiumdichloride (5 mol-%) and a compound of general formulaR⁸—B(OH)₂ (2 equivalents) in a solvent mixture of toluene/dioxane/2 Naq. sodium carbonate soln. (20 mL per 1 mmol compound of general formulaVI-A). The reaction mixture is heated to reflux for 12 hours andfiltered over Celite. The combined organic extracts are dried overmagnesium sulfate and the solvent is removed under a vacuum. The residueis purified by flash chromatography (SiO₂, different mixture of hexanesand EA).

The following compounds A-181 to A-201 were obtained according to theabove-stated general method:

A-181: 2-(4-chloro-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.29 (d, 1H, J=8.0 Hz), 7.98 (d, 2H, J=9.2 Hz), 7.76 (d, 1H, J=8.1 Hz),7.54 (d, 2H, J=8.8 Hz); IR (neat) 2220, 1593, 1493, 1454, 1404, 1340,1186, 1151, 1091, 1045, 1013, 841 cm⁻¹; MS (FAB) m/z 283 (M+H)

A-182: 6-(trifluoromethyl)-2-phenylpyridine-3-carbonitrile

¹H NMR (300 MHz, CDCl₃)

7.50-7.55 (m, 3H), 7.72 (d, 1H, J=7.8 Hz), 7.95-8.01 (m, 2H), 8.24 (d,1H, J=7.8 Hz); IR (neat) 2923, 2250, 1515, 1461, 1400, 1339, 1186, 1148cm⁻¹; MS (FAB) m/z 249 (M+H)

A-183: 2-thiophen-2-yl-6-trifluoromethyl-nicotinonitrile

¹H NMR (400 MHz, CDCl₃) δ 8.33 (d, 1H, J=2.7 Hz), 8.17 (d, 1H, J=6.0Hz), 7.61 (dd, 1H, J=7.8, 0.6 Hz), 7.58 (d, 1H, J=6.0 Hz), 7.20 (t, 1H,J=2.7 Hz); MS (FAB) m/z 255 (M+H)

A-184: 2-(4-fluoro-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.27 (d, 1H, J=8.1 Hz), 8.04 (m, 2H), 7.74 (d,1H, J=8.1 Hz), 7.24 (m, 2H); IR (neat) 3363, 2958, 1716, 1614, 1515,1457, 1344, 1247, 1143, 1050, 833 cm⁻¹; MS (FAB) m/z 267 (M+H)

A-185: 2-(4-tert-butyl-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.26 (d, 1H, J=8.1 Hz), 7.96 (d, 2H, J=9.0 Hz), 7.70 (d, 1H, J=8.1 Hz),7.54 (d, 2H, J=9.0 Hz), 1.37 (s, 9H); IR (neat) 3267, 2920, 1731, 1604,1510, 1413, 1345, 1229, 1141, 1094, 1049, 839, 749 cm⁻¹; MS (FAB) m/z306 (M+H)

A-186: 2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.29 (d, 1H, J=7.8 Hz), 8.02 (dd, 1H, J=6.9, 2.1 Hz), 7.95 (m, 1H), 7.78(d, 1H, J=7.8 Hz), 7.33 (t, 1H, J=8.4 Hz); MS (FAB) m/z 301 (M+H)

A-187: 2-(3-fluoro-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃)

8.29 (d, 1H, J=8.0 Hz), 7.82 (m, 1H), 7.78 (d, 1H, J=8.0 Hz), 7.71 (m,1H), 7.53 (m, 1H), 7.26 (m, 1H); IR (neat) 3424, 2235, 1584, 1463, 1398,1340, 1278, 1189, 1153, 1093, 1051, 918, 850, 781, 707 cm⁻¹; MS (FAB)m/z 267 (M+H)

A-188: 2-cyclohex-1-enyl-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.13 (d, 1H, J=8.1 Hz), 7.19 (d, 1H, J=8.1Hz), 6.65 (m, 1H), 2.57 (m, 2H), 2.33 (m, 2H), 1.66-1.86 (m, 4H); MS(FAB) m/z 253(M+H)

A-189: 4′-tert-butyl-5-trifluoromethyl-biphenyl-2-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.89 (d, 1H, J=7.7 Hz), 7.78 (s, 1H), 7.68 (d,1H, J=7.9 Hz), 7.54 (d, 4H, J=0.9 Hz), 1.38 (s, 9H); IR (neat) 2964,2240, 1538, 1420, 1335, 1260, 1175, 1075, 838 cm⁻¹; MS (FAB) m/z304(M+H)

A-190: 4′-methoxy-5-trifluoromethyl-biphenyl-2-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.88 (d, 1H, J=8.2 Hz), 7.75 (s, 1H), 7.66 (d,1H, J=8.0 Hz), 7.53 (dd, 2H, J=6.8 Hz, J=1.8 Hz), 7.05 (dd, 2H, J=6.6Hz, J=2.0 Hz), 3.88 (s, 3H); IR (neat) 2958, 2240, 1610, 1517, 1294,1076, 1040, 909, 831 cm⁻¹; MS (FAB) m/z 277(M+H)

A-191: 3′-chloro-5-trifluoromethyl-biphenyl-2-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.93 (d, 1H, J=8.3 Hz), 7.75 (d, 2H, J=7.7Hz), 7.53 (m, 1H), 7.45 (m, 3H); IR (neat) 3068, 2232, 1567, 1411, 1252,1041, 839, 698 cm⁻¹; MS (FAB) m/z 282(M+H)

A-192: 3′-fluoro-5-trifluoromethyl-biphenyl-2-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.92 (dd, 1H, J=7.9 Hz, J=0.6 Hz), 7.75 (m,2H), 7.52 (m, 1H), 7.37 (d, 1H, J=6.0 Hz), 7.20 (m, 2H); IR (neat) 2238,1588, 1489, 1450, 1292, 907, 841, 791, 701 cm⁻¹; MS (FAB) m/z 265(M+H)

A-193: 3′-chloro-4′-fluoro-5-trifluoromethyl-biphenyl-2-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.93 (d, 1H, J=8.2 Hz), 7.76 (d, 2H, J=7.1Hz), 7.61 (dd, 1H, J=6.8 Hz, J=2.4 Hz), 7.48 (m, 1H), 7.32 (m, 1H); IR(neat) 2238, 1490, 1416, 1333, 1263, 1177, 1075, 888, 835 cm⁻¹; MS (FAB)m/z 299(M+H)

A-194: 3′,4′-dimethoxy-5-trifluoromethyl-biphenyl-2-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.88 (d, 1H, J=8.3 Hz), 7.78 (s, 1H), 7.67 (d,1H, J=8.0 Hz), 7.14 (m, 2H), 7.01 (d, 1H, J=8.3 Hz), 3.97 (s, 3H), 3.96(s, 3H),

IR (neat) 2940, 2238, 1604, 1521, 1420, 1217, 1075, 1025, 838 cm⁻¹; MS(FAB) m/z 308(M+H)

A-195: 2-pyridin-3-yl-4-trifluoromethyl-benzonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.81 (d, 1H, J=2.2 Hz), 8.77 (dd, 1H, J=5.0Hz, J=1.7 Hz), 7.96 (m, 2H), 7.80 (d, 2H, J=5.7 Hz), 7.50 (m, 1H); IR(neat) 3031, 2238, 2229, 1569, 1415, 1015, 929, 839, 808 cm⁻¹; MS (FAB)m/z 249(M+H)

A-196: 2-(3,4-dimethoxy-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.19 (d, 1H, J=7.9 Hz), 7.62 (m, 3H), 6.98 (d,1H, J=8.4 Hz), 3.95 (s, 3H), 3.92 (s, 3H); IR (neat) 2969, 2238, 1569,1462, 1340, 1088, 1024, 845, 762 cm⁻¹; MS (FAB) m/z 309(M+H)

A-197: 2-(3,5-dimethoxy-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.23 (d, 1H, J=8.1 Hz), 7.71 (d, 1H, J=8.1Hz), 7.10 (s, 2H), 6.61 (s, 1H), 3.85 (s, 6H); IR (neat) 2233, 1598,1458, 1400, 920, 859, 831, 790 cm⁻¹; MS (FAB) m/z 309(M+H)

A-198: 3′,5′-dimethoxy-5-trifluoromethyl-biphenyl-2-carbonitrile

¹H NMR (300 MHz, CDCl₃) δ 7.80 (m, 2H), 6.95 (d, 1H, J=2.4 Hz), 6.73 (m,2H), 6.57 (m, 1H), 3.86 (s, 3H), 3.85 (s, 3H); IR (neat) 2940, 2240,1457, 1422, 1067, 905, 843, 701 cm⁻¹; MS (FAB) m/z 308(M+H)

A-199: 2-(3-chloro-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.29 (d, 1H, J=8.1 Hz), 7.96 (m, 1H), 7.90 (m,1H), 7.78 (d, 1H, J=8.0 Hz), 7.46-7.55 (m, 2H); IR (neat) 3394, 2231,1566, 1337, 1194, 1134, 1089, 850 cm⁻¹; MS (FAB) m/z 283 (M+H)

A-200: 2-(2-fluoro-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.29 (d, 1H, J=8.1 Hz), 7.83 (d, 1H, J=8.1Hz), 7.65 (m, 1H), 7.57 (m, 1H), 7.36 (dd, 1H, J=7.5, 1.1 Hz), 7.30 (m,1H); IR (neat) 2230, 1617, 1463, 1401, 1340, 1186, 1149, 852, 762 cm⁻¹;MS (FAB) m/z 267 (M+H)

A-201: 2-(4-methoxy-phenyl)-6-trifluoromethyl-nicotinonitrile

¹H NMR (300 MHz, CDCl₃) δ 8.231H, J=8.0 Hz), 8.04 (d, 2H, J=9.0 Hz),7.67 (d, 1H, J=8.0 Hz), 7.06 (d, 2H, J=9.0 Hz), 3.90 (s, 3H); IR (neat)2239, 1608, 1398, 1340, 1259, 1181, 1148, 1087, 841 cm⁻¹; MS (FAB) m/z279 (M+H)

Stage 2: Method 1

Compounds of the general formula VI-E (5 mmol), in which R⁵, R⁸, U, Tand V have the above-stated meaning and m denotes 0, 1, 2 or 3,palladium on carbon (10%, 500 mg) and concentrated hydrochloric acid (3mL) are dissolved in MeOH (30 mL) and exposed to a hydrogen atmospherefor 6 hours at RT. The reaction mixture is filtered through celite andthe filtrate is evaporated under a vacuum. The residue is purified bymeans of flash chromatography (SiO₂, EA).

The following compounds B-151 to B-152 were obtained according to theabove-stated general method:

B-151: C-(2-cyclohexyl-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.81 (d, 1H, J=7.8 Hz), 7.45 (d, 1H, J=7.8Hz), 3.99 (s, 2H), 2.87 (m, 1H), 1.72-1.88 (m, 6H), 1.44 (bs, 2H),1.34-1.37 (m, 4H); IR (neat) 2928, 2855, 1588, 1453, 1405, 1343, 1257,1179, 1137, 1011, 917, 841 cm⁻¹; MS (FAB) m/z 259(M+H)

B-152: C-(4-phenyl-6-trifluoromethyl-pyridin-3-yl)-methylamine

¹H NMR (300 MHz, CD₃OD) δ 7.76 (s, 1H), 7.18-7.55 (m, 6H), 4.27 (s, 2H)

IR (neat) 398, 2948, 1595, 1491, 1404, 1332, 1220, 1140, 1084, 919, 769,701 cm⁻¹; MS (FAB) m/z 253(M+H)

Method 2:

Compounds of the general formula VI-E (2 mmol), in which R⁵, R⁸, U, Tand V have the above-stated meaning and m denotes 0, 1, 2 or 3, aredissolved in THF (10 mL) and BH₃—S(CH₃)_(2 [)2.0 M in THF, 3 mL, 3equivalents] is added.

The reaction mixture is heated to reflux for 8 hours, aq. HCl (2 N) isadded and the reaction mixture is again heated to reflux for 30 minutes.Aq. NaOH soln. and EA are added. The combinded organic extracts arewashed with sat. aq. NaCl soln. and dried over MgSO₄. The solvent isevaporated under a vacuum and the residue is purified by flashchromatography (SiO₂, different mixtures of methylene chloride andmethanol).

The following compounds B-153 to B-171 were obtained according to theabove-stated general method:

B-153: (6-(trifluoromethyl)-2-phenylpyridin-3-yl)methanamine

¹H NMR (300 MHz, CDCl₃)

18.07 (d, 1H, J=7.8 Hz), 7.67 (d, 1H, J=7.8 Hz), 7.43-7.55 (m, 5H), 3.97((s, 2H); IR (neat) 2924, 1402, 1344, 1179, 1136, 844, 768, 702 cm⁻¹; MS(FAB) m/z 253(M+H)

B-154: (2-bromo-6-(trifluoromethyl)pyridin-3-yl)methanamine

¹H NMR (300 MHz, CDCl₃) δ 7.91 (d, 1H, J=7.8 Hz), 7.61 (d, 1H, J=7.8Hz), 3.95 (s, 2H); MS (FAB) m/z 256 (M+H)

B-155:C-[2-(4-tert-butyl-phenyl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃+CD₃OD) d 8.26 (d, 1H, J=7.8 Hz), 7.63 (d, 1H,J=7.8 Hz), 7.40 (d, 2H, J=8.1 Hz), 7.29 (d, 2H, J=8.1 Hz), 4.51 (s, 2H),1.25 (s, 9H); MS (FAB) m/z 309 (M+H)

B-156:C-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.14 (d, 1H, J=7.8 Hz), 7.65-7.71 (m, 2H), 7.46 (m, 1H), 7.23 (t, 1H,J=8.4 Hz), 3.96 (s, 2H); MS (FAB) m/z 305 (M+H)

B-157:[4-(3-aminomethyl-6-trifluoromethyl-pyridin-2-yl)-phenyl]-dimethyl-amine

¹H NMR (300 MHz, CDCl₃) δ 8.03 (d, 1H, J=7.5 Hz), 7.56 (d, 1H, J=7.5Hz), 7.47 (d, 2H, J=9.0 Hz), 6.77 (d, 2H, J=9.0 Hz), 4.06 (s, 2H), 3.01(s, 6H), 2.36 (bs, 2H); IR (neat) 3396, 2921, 1610, 1518, 1401, 1344,1176, 944, 824 cm⁻¹; MS (FAB) m/z 296 (M+H)

B-158:C-[2-(4-chloro-phenyl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.11 (d, 1H, J=8.0 Hz), 7.66 (m, 1H), 7.52 (d, 2H, J=8.2 Hz), 7.44 (d,2H, J=8.4 Hz), 3.96 (s, 2H); IR (neat) 2921, 1595, 1460, 1407, 1344,1178, 1138, 1093, 835 cm⁻¹; MS (FAB) m/z 287 (M+H)

B-159:C-[2-(3-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.12 (d, 1H, J=8.1 Hz), 7.70 (d, 1H, 8.1 Hz), 7.45 (m, 1H), 7.27-7.35(m, 2H), 7.09 (m, 1H), 3.98 (s, 2H); IR (neat) 2922, 1587, 1463, 1400,1344, 1272, 1183, 1136, 845, 792, 708 cm⁻¹; MS (FAB) m/z 271 (M+H)

B-160:C-[2-(3-chloro-phenyl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.11 (d, 1H, J=8.0 Hz), 7.70 (d, 1H, J=8.0 Hz), 7.56 (m, 1H), 7.37-7.46(m, 3H), 3.97 (s, 2H); IR (neat) 2922, 1586, 1344, 1179, 1138, 1099,888, 845 cm⁻¹; MS (FAB) m/z 287 (M+H)

B-161:C-[2-(2-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-101]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.14 (d, 1H, J=8.0 Hz), 7.74 (d, 1H, J=8.1 Hz), 7.42-7.48 (m, 2H), 7.30(m, 1H), 7.17 (m, 1H), 3.86 (s, 2H); IR (neat) 2924, 1617, 1456, 1345,1179, 1138, 762 cm⁻¹; MS (FAB) m/z 271 (M+H)

B-162:C-[2-(4-methoxy-phenyl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃)

8.06 (d, 1H, J=7.9 Hz), 7.63 (d, 1H, J=7.9 Hz), 7.52 (d, 2H, J=8.8 Hz),7.00 (d, 2H, J=8.8 Hz), 4.01 (s, 2H), 3.87 (bs, 3H); IR (neat) 2926,1611, 1515, 1345, 1251, 1178, 1135, 837 cm⁻¹; MS (FAB) m/z 283 (M+H)

B-163: C-(4′-tert-butyl-5-trifluoromethyl-biphenyl-2-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.60 (s, 2H), 7.47 (m, 3H), 7.26 (m, 2H), 3.87(s, 2H), 1.37 (s, 9H); IR (neat) 2963, 1514, 1419, 1259, 1167, 1078,1036, 836 cm⁻¹; MS (FAB) m/z 308(M+H)

B-164: C-(4′-methoxy-5-trifluoromethyl-biphenyl-2-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.59 (s, 2H), 7.48 (s, 1H), 7.25 (m, 2H), 6.98(dd, 2H, J=8.6 Hz, J=2.0 Hz), 3.86 (s, 3H); IR (neat) 3328, 2914, 1610,1516, 1464, 1418, 1042, 904 cm⁻¹; MS (FAB) m/z 282(M+H)

B-165: C-(3′-chloro-5-trifluoromethyl-biphenyl-2-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.65 (s, 2H), 7.47 (s, 1H), 7.39 (m, 2H), 7.35(m, 1H), 7.22 (m, 1H), 3.84 (s, 2H); IR (neat) 2921, 1565, 1419, 1256,1040, 835, 791, 701 cm⁻¹; MS (FAB) m/z 286(M+H)

B-166: C-(3′-fluoro-5-trifluoromethyl-biphenyl-2-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.64 (d, 2H, J=1.3 Hz), 7.48 (s, 1H), 7.41 (m,1H), 7.09 (m, 3H), 3.85 (s, 2H); IR (neat) 2920, 1615, 1485, 1444, 1274,902, 791, 705 cm⁻¹; MS (FAB) m/z 270(M+H)

B-167:C-(3′-chloro-4′-fluoro-5-trifluoromethyl-biphenyl-2-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.65 (s, 2H), 7.43 (m, 2H), 7.24 (m, 2H), 3.83(s, 2H); IR (neat) 2921, 1494, 1419, 1168, 1078, 886, 828 cm⁻¹; MS (FAB)m/z 304(M+H)

B-168: C-(3′,4′-dimethoxy-5-trifluoromethyl-biphenyl-2-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.60 (d, 2H, J=1.3 Hz), 7.50 (s, 1H), 6.94 (m,1H), 6.88 (m, 2H), 3.94 (s, 3H), 3.90 (s, 3H), 3.69 (m, 2H); IR (neat)3367, 2938, 1518, 1421, 1170, 1078, 1026, 816 cm⁻¹; MS (FAB) m/z312(M+H)

B-169:C-[2-(3,4-dimethoxy-phenyl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 8.06 (d, 1H, J=7.9 Hz), 7.64 (d, 1H, J=7.9Hz), 7.16 (d, 1H, J=2.0 Hz), 7.12 (dd, 1H, J=8.1 Hz, J=2.0 Hz), 6.96 (d,1H, J=8.3 Hz), 4.01 (s, 2H), 3.94 (s, 3H), 3.93 (s, 3H); IR (neat) 2937,1604, 1463, 1415, 1253, 1175, 1026, 819 cm⁻¹; MS (FAB) m/z 313(M+H)

B-170:C-[2-(3,5-dimethoxy-phenyl)-6-trifluoromethyl-pyridin-3-yl]-methylamine

¹H NMR (300 MHz, CDCl₃) δ 8.07 (d, 1H, J=8.0 Hz), 7.67 (d, 1H, J=8.0Hz), 6.65 (d, 2H, J=1.8 Hz), 6.53 (t, 1H, J=2.2 Hz), 3.96 (s, 2H), 3.82(s, 6H); IR (neat) 2942, 1597, 1460, 1401, 1345, 1098, 1040, 841 cm⁻¹;MS (FAB) m/z 313(M+H)

B-171: C-(3′,5′-dimethoxy-5-trifluoromethyl-biphenyl-2-yl)-methylamine

¹H NMR (300 MHz, CDCl₃) δ 7.60 (s, 2H), 7.50 (s, 1H), 6.50 (t, 1H, J=2.4Hz), 6.46 (d, 2H, J=2.4 Hz), 3.87 (s, 2H), 3.82 (s, 6H); IR (neat) 2940,1458, 1417, 1332, 1207, 1077, 903, 837 cm⁻¹; MS (FAB) m/z 312(M+H)

6. General Procedure for the Preparation of Carbonic Acids of GeneralFormula VIIa

Carbonic acids of the general formula VIIIa are prepared as shown inscheme 5 below.

Stage 1:

Compounds of general formula XI (7 mmol), wherein R¹, R², R³, R⁴ and Yhave the above-stated meaning and R denotes a linear or branchedC₁₋₆-alkyl residue, are treated with a compound of general formulaCl—S(═O)₂—Y (8 mmol), wherein Y has the above-stated meaning. Thereaction mixture is stirred for 10 min at 0° C. and subsequently for 3hours at room temperature in pyridine (10 mL). The reaction mixture istaken up in methylene chloride and aq. HCl (1 N). The organic phase isseparated and the solvent is removed under a vacuum. The residue is ineach case crystallized from mixtures of methylene chloride and hexanes.

Stage 2:

Compounds of general formula XII (5 mmol), wherein R¹, R², R³, R⁴ and Yhave the above-stated meaning and R denotes a linear or branchedC₁₋₆-alkyl residue, are treated with lithiumhydroxide monohydrate (15mmol) in a solvent mixture of water and tetrahydrofuran (1:2, 24 mL) for4 hours at 40° C. The reaction mixture is taken up in dichloromethaneand water, treated with aq. HCl (1 N), and repeatedly extracted withdichloromethane. The combined organic extracts are washed with sat. aq.NaCl soln. and dried over sodium sulfate. The solvent is removed under avacuum and the residue is in each case crystallized from mixtures ofmethylene chloride and hexanes.

D-1: 2-(4-dimethylaminosulfonylamino-3-fluoro-phenyl)-propionic acidethylester

¹H NMR (300 MHz, CDCl₃)

7.44 (dd, 1H, J=8.1, 8.1 Hz), 6.94-7.05 (m, 2H), 6.78 (bs, 1H), 4.07 (m,2H), 3.62 (q, 1H, J=6.9 Hz), 2.76 (s, 6H), 1.39 (d, 3H, J=6.9 Hz), 1.39(t, 3H, J=7.2 Hz), 1.17 (t, 3H, J=7.5 Hz) MS (FAB) m/z 319(M+H)

D-2: 2-(4-dimethylaminosulfonylamino-3-fluoro-phenyl)-propionic acid

¹H NMR (300 MHz, CDCl₃)

750 (dd, 1H, J=8.1, 8.1 Hz), 7.05-7.12 (m, 2H), 6.69 (bs, 1H), 3.71 (q,1H, J=6.9 Hz), 2.82 (s, 6H), 1.49 (d, 3H, J=6.9 Hz) MS (FAB) m/z291(M+H)

D-3:2-[3-fluoro-4-(2,2,2-trifluoro-ethansulfonylamino)-phenyl]-propionicacid ethyl ester

¹H NMR (300 MHz, CDCl₃)

7.50 (dd, 1H, J=8.1, 8.1 Hz), 7.11-7.18 (m, 2H), 7.00 (bs, 1H), 4.14 (m,2H), 3.87 (q, 2H, J=9.0 Hz), 3.70 (q, 1H, J=6.9 Hz), 1.49 (d, 3H, J=6.9Hz), 1.23 (t, 3H, J=6.9 Hz)

MS (FAB) m/z 358 (M+H)

D-4:2-[3-fluoro-4-(2,2,2-trifluoro-ethansulfonylamino)-phenyl]-propionicacid

MS (FAB) m/z 330 (M+H)

D-5: 2-(3-fluoro-4-trifluoromethylsulfonamido-phenyl)-propionic acidethyl ester

¹H NMR (300 MHz, CDCl₃)

7.45 (dd, 1H, J=8.1, 8.1 Hz), 7.09-7.16 (m, 2H), 7.00 (bs, 1H), 4.14 (m,2H), 3.70 (q, 1H, J=6.9 Hz), 1.49 (d, 3H, J=6.9 Hz), 1.22 (t, 3H, J=7.2Hz); MS (FAB) m/z 344 (M+H)

D-6: 2-(4-aminosulfonylamino-3-fluoro-phenyl)-propionic acid

¹H NMR (300 MHz, CDCl₃) δ 7.49 (dd, 1H, J=8.1, 8.1 Hz), 7.04-7.12 (m,2H), 6.68 (bs, 1H), 5.05 (bs, 2H), 4.14 (m, 2H), 3.68 (q, 1H, J=6.9 Hz),1.46 (d, 3H, J=6.9 Hz), 1.23 (t, 3H, J=7.2 Hz)

MS (FAB) m/z 291(M+H)

D-7:2-[3-fluoro-4-(2,2,2-trifluoro-ethansulfonylamino)-phenyl]-propionicacid

MS (FAB) m/z 330 (M+H)

D-8: 2-[3-fluoro-4-(propan-2-sulfonylamino)-phenyl]-propionic acidethylester

¹H NMR (300 MHz, CDCl₃)

7.55 (dd, 1H, J=8.1, 8.1 Hz), 7.05-7.12 (m, 2H), 6.71 (bs, 1H), 4.15 (m,2H), 3.67 (q, 1H, J=6.9 Hz), 3.07 (m, 1H), 1.47 (d, 3H, J=6.9 Hz), 1.40(d, 6H, J=6.9 Hz), 1.22 (t, 3H, J=7.2 Hz)

MS (FAB) m/z 318(M+H)

D-9: 2-(4-ethanesulfonylamino-3-fluoro-phenyl)-propionic acid ethylester

¹H NMR (300 MHz, CDCl₃)

7.52 (dd, 1H, J=8.1, 8.1 Hz), 7.06-7.14 (m, 2H), 6.62 (bs, 1H), 4.13 (m,2H), 3.66 (q, 1H, J=6.9 Hz), 3.12 (q, 2H, J=7.2 Hz), 1.47 (d, 3H, J=6.9Hz), 1.39 (t, 3H, J=7.2 Hz), 1.2 5(t, 3H, J=7.2 Hz)

MS (FAB) m/z 304(M+H)

D-10: 2-(4-ethanesulfonylamino-3-fluoro-phenyl)-propionic acid

¹H NMR (300 MHz, CDCl₃) δ 7.53 (dd, 1H, J=8.1, 8.1 Hz), 7.08-7.15 (m,2H), 6.76 (bs, 1H), 3.71 (q, 1H, J=6.9 Hz), 3.12 (q, 2H, J=7.5 Hz), 1.50(d, 3H, J=6.9 Hz), 1.39 (t, 3H, J=7.5 Hz)

MS (FAB) m/z 276(M+H)

Compounds of general formula VIIa, in which R² denotes methyl, can beprepared according to the following procedures.

To a stirred solution of potassium t-butoxide (125.7 g, 1.12 mol) in DMF(600 mL) was added a mixture of 1-bromo-2-nitrobenzene (56.5 g, 0.28mol) and ethyl 2-chloropropionate (38.7 g, 0.28 mol) at −30° C. within 3min. After being stirred for 2 min at −30° C., more ethyl2-chloropropionate (3.87 g, 0.028 mol) was added. After being stirredfor 5 min at −30° C. the mixture was poured into cooled 10% aq. HClsoln., diluted with water and extracted with EA several times. Thecombined organic layers were washed with water and brine, dried overMgSO₄, and concentrated in vacuo. The residue was purified by flashcolumn chromatography on silica gel using EA:hexanes (1:10) as eluent. I

To a stirred solution of ethyl 2-(3-bromo-4-nitrophenyl)propanoate (3.76g, 0.012 mol) in DMF (20 mL) under nitrogen was added a Pd(PPh₃)₄ (0.77g, 5 mol %) and tetramethyltin (6.68 g, 0.037 mol) at rt. After beingstirred for 8 hrs at 120° C. the mixture was cooled to rt and thenfiltered through Celite. The filtrate was diluted with water andextracted with EA several times. The combined organic layers were washedwith water and brine, dried over MgSO₄, and concentrated in vacuo. Theresidue was purified by flash column chromatography on silica gel usingEA:hexanes (1:10) as eluent.

A suspension of ethyl 2-(3-methyl-4-nitrophenyl)propanoate (1.76 g,0.007 mol) and 10% Pd on carbon (200 mg) in MeOH (30 mL) washydrogenated under a balloon of hydrogen for 6 hrs and filtered throughcelite. The filtrate was concentrated in vacuo and the residue waspurified by flash column chromatography on silica gel using EA/hexanes(1:4) as eluent. The compound thus obtained (1.43 g, 0.007 mol) andmethanesulfonyl chloride (0.95 g, 0.008 mol) in pyridine (10 mL) werestirred at 0° C. for 10 min then stirred for 3 hrs at rt. After removingpyridine by 1 N HCl/dichloromethane workup, the organic layer wasconcentrated in vacuo. The residue was purified by recystallization withdichloromethane/n-hexane.

7. General Method for Reacting Amines of the General Formulae V or Xwith Carboxylic Acids of the General Formula VII

The acid of the general formula VII (1 equivalent), the amine of thegeneral formulae V or X (1.2 equivalents) and EDCI (1.2 equivalents) arestirred in DMF (10 mmol acid in 20 mL) for 12 hours at RT and water isthen added. The reaction mixture is repeatedly extracted with EA, theaqueous phase is saturated with NaCl and then extracted again with EA.The combined organic phases are washed with 1 N hydrochloric acid andsat. aq. NaCl soln., dried over MgSO₄ and the solvent is removed under avacuum. The residue is purified by means of flash chromatography (SiO₂,EA/hexane 1:2).

The following example compounds 1, 2, 3, 10, 12, 13, 33 and 34 wereobtained according to the above-stated general method:

Example 22-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide

The compound was obtained in a yield of 88% as a white solid with amelting point of 75-79° C.

¹H NMR (300 MHz, CDCl₃) δ 7.47-7.55 (m, 2H, Ar), 7.07-7.22 (m, 3H, Ar),6.33 (bt, 1H, NHCO), 4.47 (d, 2H, J=5.7 Hz, ArCH₂NH), 3.54 (q, 1H, J=6.9Hz, CHCH₃), 3.00-3.05 (m, 7H, piperidine, SO₂CH₃), 1.61 (m, 6H,piperidine), 1.52 (d, 3H, J=6.9 Hz, CHCH₃)

IR (KBr) 3741, 3281, 2935, 1652, 1512, 1419, 1334, 1248 cm⁻¹

MS (FAB) m/z 503 (M+H)

Example 10(S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide

The compound was obtained in a yield of 65% as a white solid with amelting point of 75-79° C.

¹H NMR (300 MHz, CDCl₃)

7.47-7.55 (m, 2H, Ar), 7.07-7.22 (m, 3H, Ar), 6.33 (bt, 1H, NHCO), 4.47(d, 2H, J=5.7 Hz, ArCH₂NH), 3.54 (q, 1H, J=6.9 Hz, CHCH₃), 3.00-3.05 (m,7H, piperidine, SO₂CH₃), 1.52 (d, 3H, J=6.9 Hz, CHCH₃), 1.61 (m, 6H,piperidine)

IR (KBr) 3289, 2935, 2853, 1655, 1591, 1512, 1419, 1335 cm⁻¹

MS (FAB) m/z 503 (M+H)

Example 122-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-morpholino-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide

The compound was obtained in a yield of 60% as a white solid.

¹H NMR (300 MHz, CDCl₃)

7.49-7.56 (m, 2H, Ar), 7.26 (d, 1H, J=7.5 Hz, Ar), 7.08-7.17 (m, 2H,Ar), 6.53 (bs, 1H, NHSO₂), 6.06 (bt, 1H, NHCO), 4.48 (d, 2H, J=5.7 Hz,ArCH₂NH), 3.76 (m, 4H, Morpholin), 3.57 (q, 1H, J=6.9 Hz, CHCH₃), 3.13(m, 4H, morpholine), 3.04 (s, 3H, SO₂CH₃), 1.55 (d, 3H, J=6.9 Hz, CHCH₃)

IR (KBr) 3741, 1645, 1512, 1416, 1334, 1157 cm⁻¹

MS (FAB) m/z 505 (M+H)

Example 132-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide

The product was obtained in a yield of 80%.

¹H NMR (300 MHz, CDCl₃)

7.51 (t, 1H, J=8.3 Hz, H-5), 7.38 (d, 2H, J=7.5 Hz Ar), 7.13 (dd, 1H,J=11.1, 2.0 Hz, Ar), 7.07 (dd, 1H, J=7.8, 1.8 Hz, Ar), 6.94 (d, 1H,J=7.5 Hz, Ar), 5.72 (bt, 1H, NHCO), 4.47 (d, 2H, J=5.3 Hz, ArCH₂NH),3.52 (q, 1H, J=6.9 Hz, CHCH₃), 3.42-3.46 (m, 4H, pyrrolidine), 3.02 (s,3H, SO₂CH₃), 1.82-1.89 (m, 4H, pyrrolidine), 1.50 (d, 3H, J=6.9 Hz,CHCH₃)

Example 12-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-methyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide

The compound was obtained in a yield of 78% as a white solid with amelting point of 149-152° C.

¹H NMR (300 MHz, CDCl₃)

7.54 (d, 1H, J=7.8 Hz, Ar), 7.41-7.46 (m, 2H, Ar), 7.14 (dd, 1H, J=11.1,2.0 Hz, Ar), 7.07 (dd, 1H, J=7.8, 1.8 Hz, Ar), 6.87 (bs, 1H, NHSO₂),6.16 (bt, 1H, NHCO), 4.43 (d, 2H, J=5.1 Hz, ArCH₂NH), 3.58 (q, 1H, J=6.9Hz, CHCH₃), 3.01 (s, 3H, SO₂CH₃), 2.50 (s, 3H, ArCH₃), 1.50 (d, 3H,J=6.9 Hz, CHCH₃)

IR (KBr) 3741, 1649, 1513, 1338, 1153, 756 cm⁻¹

MS (FAB) m/z 434 (M+H)

Example 32-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide

The compound was obtained in a yield of 78% as a pale yellow solid witha melting point of 126-127° C.

¹H NMR (300 MHz, CDCl₃)

7.48 (t, 1H, J=8.3 Hz, H-5), 7.32 (bd, 2H, Ar), 7.05-7.15 (m, 4H, Ar),6.81 (bs, 1H, NHSO₂), 6.66 (bt, 1H, NHCO), 4.52 (d, 2H, J=5.1 Hz,ArCH₂NH), 3.55 (q, 1H, J=6.9 Hz, CHCH₃), 3.00 (s, 3H, SO₂CH₃), 2.79 (bs,4H, piperidine), 1.49-1.64 (m, 7H, piperidine, CHCH₃), 1.25 (m, 2H,piperidine)

IR (KBr) 3289, 2934, 1652, 1511, 1423, 1337, 1220, 1160 cm⁻¹

MS (FAB) m/z 502 (M+H)

Example 332-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-morpholino-4-(trifluoromethyl)benzyl)propanamide

The compound was obtained in a yield of 60% as a white solid.

¹H NMR (300 MHz, CDCl₃)

7.43 (t, 1H, J=8.3 Hz, Ar), 7.16-7.24 (m, 3H, Ar), 7.09 (dd, 1H, J=11.1,2.0 Hz, Ar), 7.01 (dd, 1H, J=7.8, 1.8 Hz, Ar), 6.70 (bs, 1H, NHSO₂),6.15 (bt, 1H, NHCO), 4.47 (d, 2H, J=5.4 Hz, ArCH₂NH), 3.70 (t, 4H, J=4.2Hz, morpholine), 3.50 (q, 1H, J=7.2 Hz, CHCH₃), 2.95 (s, 3H, SO₂CH₃),2.78 (t, 4H, J=4.2 Hz, morpholine), 1.45 (d, 3H, J=7.2 Hz, CHCH₃)

IR (KBr) 2921, 1650, 1512, 1423, 1336, 1159 cm⁻¹

MS (FAB) m/z 504 (M+H)

Example 342-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide

The product was obtained in a yield of 70%.

¹H NMR (300 MHz, CDCl₃)

7.49 (t, 1H, J=8.1 Hz, Ar), 7.05-7.19 (m, 5H, Ar), 6.79 (bs, 1H, NHSO₂),6.26 (bt, 1H, NHCO), 4.49 (d, 2H, J=4.8 Hz, ArCH₂NH), 3.54 (q, 1H, J=7.2Hz, CHCH₃), 3.08-3.12 (m, 4H, pyrrolidine), 3.01 (s, 3H, SO₂CH₃),1.86-1.90 (m, 4H, pyrrolidine), 1.50 (d, 3H, J=7.2 Hz, CHCH₃)

The compounds listed in Table 1 may also be obtained as described above.The starting compounds required for this purpose are known to the personskilled in the art.

TABLE 1  [4]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-fluoro-6-(trifluoromethyl)-pyridin-3-yl)methyl)propanamide  [5]N-(2-chloro-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide  [6]N-(2-bromo-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide  [7]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-iodo-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide  [8]N-(2-tert-butyl-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide  [9]N-(2-cyano-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [11](R)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [14]N-(2-(dimethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [15]N-(2-(diethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [16]N-(2-(dipropylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [17]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-hydroxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [18]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-methoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [19]N-(2-butoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [20]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-isopropoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [21]N-(2-cyclopentyloxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [22]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-phenyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [23]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(4-fluorophenyl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [24]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(6-(trifluoromethyl)-2,2′-bipyridin-3-yl)methyl)propanamide [25]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(6-(trifluoromethyl)-2,3′-bipyridin-3-yl)methyl)propanamide [26]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrimidin-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [27]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(thiazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [28]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(oxazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [29]N-(2-(1H-imidazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [30]N-(2-cyano-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide[31](S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [32](R)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [35]N-(2-(dimethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [36]N-(2-(diethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [37]N-(2-(dipropylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [38]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-hydroxy-4-(trifluoromethyl)benzyl)propanamide[39]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-methoxy-4-(trifluoromethyl)benzyl)propanamide[40]N-(2-butoxy-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide[41] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-isopropoxy-4-(trifluoromethyl)benzyl)propanamide [42]N-(2-(cyclopentyloxy)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [43]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide [44]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(4′-fluoro-5-(trifluoromethyl)-biphenyl-2-yl)methyl)propanamide [45]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-2-yl)-4-(trifluoromethyl)benzyl)propanamide [46]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-3-yl)-4-(trifluoromethyl)benzyl)propanamide [47]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrimidin-2-yl)-4-(trifluoromethyl)benzyl)propanamide [48]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(thiazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide [49]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(oxazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide [50]N-(2-(1H-imidazol-2-yl)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [51]N-(6-tert-butyl-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsufonamido)phenyl)propanamide [52]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(4-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [53]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(3-(piperidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide [54]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(4-(piperidin-1-yl)-2-(trifluoromethyl)pyrimidin-5-yl)methyl)propanamide [55]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(3-(piperidin-1-yl)-5-(trifluoromethyl)pyrazin-2-yl)methyl)propanamide [56]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(4-(piperidin-1-yl)-6-(trifluoromethyl)pyridazinyl-3-yl)methyl)propanamide [57]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)propanamide [58]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-piperidin-1-yl)-4-(trifluoromethyl)phenyl)propanamide [59]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)ethyl)propanamide [60]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenethyl)propanamide [61]N-(2-amino-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide[62]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-nitro-4-(trifluoromethyl)-benzyl)propanamide[63]N-(4-tert-butyl-2-(piperidin-1-yl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide[64] 2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [65]2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [66]2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [67]2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [68]2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [69]2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [70]N-(4-tert-butyl-2-cyanobenzyl)-2-(3-fluoro-4-(methylsulfonamido)-phenyl)propanamide [4]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-fluoro-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide  [5]N-(2-chloro-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide  [6]N-(-bromo2-bromo-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide  [7]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-iodo-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide  [8]N-(2-tert-butyl-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide  [9]N-(2-cyano-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [11](R)-2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [14]N-(2-(dimethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [15]N-(2-(diethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [16]N-(2-(dipropylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [17]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-hydroxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [18]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-methoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [19]N-(2-butoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [20]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-isopropoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [21]N-(2-cyclopentyloxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [22]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-phenyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [23]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(4-fluoro-phenyl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [24]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(6-(trifluoromethyl)-2,2′-bipyridin-3-yl)methyl)propanamide [25]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(6-(trifluoromethyl)-2,3′-bipyridin-3-yl)methyl)propanamide [26]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(pyrimidin-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [27]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(thiazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [28]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(oxazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [29]N-(2-(1H-imidazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [30]N-(2-cyano-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [31](S)-2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [32](R)-2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [35]N-(2-(dimethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [36]N-(2-(diethylamino)-4-(trifluormethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [37]N-(2-(dipropylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [38]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-hydroxy-4-(trifluoromethyl)benzyl)propanamide[39] 2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-methoxy-4-(trifluoromethyl)benzyl)propanamide [40]N-(2-butoxy-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide[41] 2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-isopropoxy-4-(trifluoromethyl)benzyl)propanamide [42]N-(2-(cyclopentyloxy)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [43]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide [44]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(4′-fluoro-5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide [45]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-2-yl)-4-(trifluoromethyl)benzyl)propanamide [46]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-3-yl)-4-(trifluoromethyl)benzyl)propanamide [47]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(pyrimidin-2-yl)-4-(trifluoromethyl)benzyl)propanamide [48]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(thiazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide [49]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(oxazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide [50]N-(2-(1H-imidazol-2-yl)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [51]N-(6-tert-butyl-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsufonamido)phenyl)propanamide [52]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(4-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [53]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(3-(piperidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide [54]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(4-(piperidin-1-yl)-2-(trifluoromethyl)pyrimidin-5-yl)methyl)propanamide [55]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(3-(piperidin-1-yl)-5-(trifluoromethyl)pyrazin-2-yl)methyl)propanamide [56]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(4-(piperidin-1-yl)-6-(trifluoromethyl)pyridazin-3-yl)methyl)propanamide [57]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)propanamide [58]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-piperidin-1-yl)-4-(trifluoromethyl)phenyl)propanamide [59]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)ethyl)propanamide [60]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenethyl)propanamide [61]N-(2-amino-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide[62]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-nitro-4-(trifluoromethyl)benzyl)propanamide[63]N-(4-tert-butyl-2-(piperidin-1-yl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide[64]2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [65]2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [66]2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [67]2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [68]2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [69]2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [70]N-(4-tert-butyl-2-cyanobenzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide[71]N-(6-(chlorodiflouromethyl)-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-(4-methylsulfonamido)phenyl)propanamide [72](S)-2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-morpholino-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [73]N-(2-(4-benzylpiperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [74]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-piperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [75]N-(2-chloro-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide[76]N-(2-(cyclohexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [77]N-(3-chloro-5-(trifluoromethyl)pyridin-2-yl)methyl-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [78]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(3-(pyrrolidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide [79]N-(2-(3,5-dimethylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [80]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [81]N-(2-(azepan-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [82]2-(3-Fluor-4-(methylsulfonamido)phenyl)-N-(2-(4-methylpiperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide

Example compounds 8, 9, 23, 24, 25, 26, 27, 28, 29, 30, 35, 36, 38, 39,47, 48, 49, 50, 52, 54 55, 56, 59 and 60 can be obtained by thoseabove-stated methods.

Example 81N-(2-azepan-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.52 (dd, 1H, J=8.1, 8.1 Hz), 7.40 (d, 1H, J=7.5 Hz), 7.14 (dd, 1H,J=8.1, 1.8 Hz), 7.08 (d, 1H, J=8.1 Hz), 7.03 (d, 1H, J=7.5 Hz), 5.86(bt, 1H), 4.43 (d, 2H, J=5.7 Hz), 3.54 (q, 1H, J=6.9 Hz), 3.38 (m, 4H),3.03 (s, 3H), 1.75 (m, 4H), 1.57 (m, 4H), 1.52 (d, 3H, J=6.9 Hz); IR(KBr) 3291, 2928, 1652, 1593, 1511, 1422, 1333, 1275, 1214, 1159, 972,822, 759 cm⁻¹; MS (FAB) m/z 531 (M+H)

Example 802-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-4-methylpiperidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47-7.55 (m, 2H), 7.07-7.22 (m, 3H), 6.29 (bt, 1H), 4.47 (d, 2H, J=5.7Hz), 3.54 (q, 1H, J=6.9 Hz), 3.30 (m, 2H), 3.03 (s, 3H), 2.82 (m, 2H),1.71 (m, 2H), 1.52 (d, 3H, J=6.9 Hz), 1.24 (m, 3H), 0.97 (d, 3H, J=6.6Hz); IR (KBr) 3290, 2924, 1655, 1592, 1512, 1456, 1419, 1334, 1157, 970,834, 758 cm⁻¹; MS (FAB) m/z 517 (M+H)

Example 79 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-3, 5dimethylpiperidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47-7.54 (m, 2H), 7.21 (d, 1H, J=7.8 Hz), 7.13 (dd, 1H, J=8.1, 1.8 Hz),7.07 (d, 1H, J=8.1 Hz), 6.48 (bs, 1H), 6.28 (bt, 1H), 4.47 (d, 2H, J=5.7Hz), 3.54 (q, 1H, J=6.9 Hz), 3.23 (m, 2H), 3.03 (s, 3H), 2.35 (m, 2H),1.54-1.76 (m, 2H), 1.52 (d, 3H, J=6.9 Hz), 0.90 (d, 3H, J=5.7 Hz), 0.88(d, 3H, J=5.7 Hz); IR (KBr) 3289, 2957, 1655, 1591, 1512, 1458, 1419,1336, 1247, 1158, 1013, 970, 831, 757 cm⁻¹; MS (FAB) m/z 531 (M+H)

The following compounds were also prepared according to the above-statedmethod.

Example 85N-(2-dimethylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.46-7.40 (m, 2H), 7.20-7.00 (m, 3H), 6.60 (bt, 1H), 4.50 (bd, 2H), 3.60(m, 1H), 3.00 (s, 3H), 2.80 (s, 6H), 1.49 (d, 3H, J=7.0 Hz); IR (KBr)3284, 2936, 1656, 1594, 1511, 1395, 1335 cm⁻¹; MS (FAB) m/z 463 (M+H)

Example 872-(3-fluoro-4-methylsulfonamido-phenyl)-N-((6-(trifluoromethyl)-2-(1H-imidazol-1-yl)pyridin-3-yl)methyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.98 (d, 1H, J=8.4 Hz), 7.82 (s, 1H), 7.70 (d, 1H, J=8.4 Hz), 7.49 (dd,1H, J=8.1, 8.1 Hz), 7.30 (s, 1H), 7.18 (s, 1H), 7.04-7.08 (m, 2H), 6.15(bt, 1H), 4.45 (d, 2H, J=5.1 Hz), 3.53 (q, 1H, J=6.9 Hz), 3.04 (s, 3H),1.47 (d, 3H, J=6.9 Hz); IR (KBr) 2923, 1665, 1511, 1424, 1337, 1154,973, 760 cm⁻¹; MS (FAB) m/z 487 (M+H)

Example 882-(3-fluoro-4-methylsulfonamido-phenyl)-N-((6-(trifluoromethyl)-2-(thiophen-2-yl)pyridin-3-yl)methyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.74 (d, 1H, J=8.7 Hz), 7.47-7.5 (m, 3H), 7.35 (dd, 1H, 3.6, 1.2 Hz),7.02-7.11 (m, 3H), 6.51 (bs, 1H), 5.79 (bt, 1H), 4.70 (d, 2H, J=5.1 Hz),3.53 (q, 1H, J=6.9 Hz), 3.02 (s, 3H), 1.51 (d, 3H, J=6.9 Hz); IR (KBr)2920, 1737, 1644, 1509, 1428, 1328, 1148, 979, 768 cm⁻¹; MS (FAB) m/z502 (M+H)

Example 892-(3-fluoro-4-methylsulfonamido-phenyl)-N-((2-(trifluoromethyl)-6-phenylpyridin-4-yl)methyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.77 (d, 1H, J=8.1 Hz), 7.61 (d, 1H, J=8.1 Hz), 7.50 (dd, 1H, J=8.1, 8.1Hz), 7.40-7.45 (m, 2H), 6.99-7.16 (m, 4H), 6.57 (bs, 1H), 5.63 (bt, 1H),4.49 (d, 2H, J=5.7 Hz), 3.47 (q, 1H, J=6.9 Hz), 3.02 (s, 3H), 1.49 (d,3H, J=6.9 Hz); IR (KBr) 3296, 1657, 1513, 1457, 1411, 1340, 1156, 1048,973, 842, 757 cm⁻¹; MS (FAB) m/z 514 (M+H)

Example 90N-(2-cyclohexylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.51 (dd, 1H, J=6.6, 6.6 Hz), 7.22 (d, 1H, J=5.8 Hz),7.18 (dd, 1H, J=8.9, 1.5 Hz), 7.08 (d, 2H, J=6.6 Hz), 6.74 (d, 1H, J=5.8Hz), 6.47 (bs, NH), 5.84 (bd, NH), 5.67 (bt, NH), 4.32 (m, 2H), 3.91 (m,1H), 3.48 (q, 1H, J=5.7 Hz), 3.03 (s, 3H), 1.98-1.61 (m, 5H), 1.52 (d,3H, J=5.7 Hz), 1.42-1.07 (m, 5H); IR (neat) 3337, 2930, 2854, 1647,1514, 1453, 1334, 1159, 909 cm⁻¹; MS (FAB) m/z 517 (M+H)

Example 912-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.57 (d, 1H, J=7.1 Hz), 7.52 (dd, 1H, J=8.3, 8.3 Hz),7.19 (d, 1H, J=7.3 Hz), 7.12-7.05 (m, 2H), 6.48 (bs, NH), 5.99 (bt, NH),4.38-4.29 (m, 4H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s, 3H), 1.75-1.68 (m,2H), 1.49 (d, 3H, J=7.1 Hz), 1.38-1.30 (m, 6H), 0.91 (t, 3H); IR (neat)3292, 2930, 1654, 1514, 1463, 1425, 1338, 1269, 1155, 973 cm⁻¹; MS (FAB)m/z 520 (M+H)

Example 952-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.58 (d, 1H, J=7.3 Hz), 7.51 (dd, 1H, J=8.4, 8.4 Hz),7.19 (d, 1H, J=7.5 Hz), 7.12-7.05 (m, 2H), 6.50 (bs, NH), 5.95 (bt, NH),4.41-4.37 (m, 2H), 4.17-4.06 (m, 2H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s,3H), 2.05 (m, 1H), 1.49 (d, 3H, J=7.1 Hz), 0.99 (d, 6H, J=6.8 Hz); IR(neat) 3295, 2966, 1655, 1514, 1463, 1425, 1336, 1157 cm⁻¹; MS (FAB) m/z492 (M+H)

Example 100N-(2-cyclopropylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.59 (d, 1H, J=7.3 Hz), 7.51 (dd, 1H, J=8.3, 8.3 Hz),7.19 (d, 1H, J=7.5 Hz), 7.13-7.06 (m, 2H), 6.49 (bs, NH), 6.08 (bt, NH),4.42-4.39 (m, 2H), 4.24-4.11 (m, 2H), 3.52 (q, 1H, J=7.1 Hz), 3.03 (s,3H), 1.59 (d, 3H, J=7.0 Hz), 1.25-1.15 (m, 1H), 0.62-0.56 (m, 2H),0.36-0.33 (m, 2H); IR (neat) 3288, 1655, 1513, 1427, 1376, 1335, 1158,984 cm⁻¹; MS (FAB) m/z 490 (M+H)

Example 101N-(2-cyclobutylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.57 (d, 1H, J=7.5 Hz), 7.50 (dd, 1H, J=8.2, 8.2 Hz),7.19 (d, 1H, J=7.3 Hz), 7.12-7.04 (m, 2H), 6.64 (bs, NH), 6.02 (bt, NH),4.45-4.26 (m, 4H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s, 3H), 2.71 (m, 1H),2.13-1.79 (m, 6H), 1.48 (d, 3H, J=7.1 Hz); IR (neat) 3289, 2940, 1656,1513, 1424, 1335, 1157, 993 cm⁻¹; MS (FAB) m/z 504 (M+H)

Example 1022-(3-chloro-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-6trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.60 (d, 1H, J=8.4 Hz), 7.41 (s, 1H) 7.39 (d, 1H, J=7.9 Hz), 7.22 (d,1H, J=8.4 Hz), 6.95 (d, 1H, J=7.5 Hz), 6.79 (bs, 1H), 5.74 (bt, 1H),4.47 (d, 2H, J=5.1 Hz), 3.52 (q, 1H, J=7.1 Hz), 3.48-3.41 (m, 4H), 3.01(s, 3H), 1.89-1.82 (m, 4H), 1.51 (d, 3H, J=7.0 Hz); IR (neat) 3291,2974, 1651, 1598, 1497, 1431, 1333, 1159, 971, 913, 733 cm⁻¹; MS (FAB)m/z 505 (M+H)

Example 1032-(3-bromo-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.60 (d, 1H, J=8.4 Hz), 7.56 (d, 1H, J=2.0 Hz), 7.39 (d, 1H, J=7.5 Hz),7.27 (dd, 1H, J=8.3, 2.2 Hz), 6.95 (d, 1H, J=7.5 Hz), 6.77 (bs, 1H),5.77 (bt, 1H), 4.47 (d, 2H, J=5.1 Hz), 3.51 (q, 1H, J=7.1 Hz), 3.47-3.41(m, 4H), 3.01 (s, 3H), 1.89-1.83 (m, 4H), 1.51 (d, 3H, J=7.1 Hz); IR(neat) 3294, 2973, 1651, 1598, 1494, 1431, 1333, 1159, 971, 912, 733cm⁻¹; MS (FAB) m/z 549 (M+H)

Example 104N-(4-benzyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.53 (dd, 1H, J=8.2, 8.2 Hz), 7.48 (d, 1H,J=7.9 Hz), 7.29-7.14 (m, 7H), 7.07 (d, 1H, J=8.1 Hz), 6.49 (bs, 1H),6.23 (bt, 1H), 4.46 (d, 2H, J=5.7 Hz), 3.54 (q, 1H, J=7.0 Hz), 3.31 (m,2H), 3.02 (s, 3H), 2.78 (m, 2H), 2.59 (d, 2H, J=6.6 Hz), 1.78-1.71 (m,3H), 1.52 (d, 3H, J=7.1 Hz), 1.30 (m, 2H); IR (neat) 3292, 2923, 1655,1592, 1512, 1420, 1335, 1158, 968, 939, 734 cm⁻¹; MS (FAB) m/z 593 (M+H)

Example 106N-(2-benzyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.62 (d, 1H, J=7.1 Hz), 7.47 (dd, 1H, J=8.4, 8.4 Hz), 7.44-7.36 (m, 5H),7.24 (d, 1H, J=7.5 Hz), 7.04 (dd, 1H, J=11.2, 1.8 Hz), 6.97 (d, 1H,J=8.4 Hz), 6.42 (bs, 1H), 5.96 (bt, 1H), 5.41 (m, 2H), 4.39 (m, 2H),3.41 (q, 1H, J=7.1 Hz), 3.01 (s, 3H), 1.42 (d, 3H, J=7.1 Hz); IR (neat)3295, 1655, 1512, 1419, 1353, 1267, 1156, 977, 907, 737 cm⁻¹; MS (FAB)m/z 526 (M+H)

Example 1072-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methoxy-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.62 (d, 1H, J=7.7 Hz), 7.46 (dd, 1H, J=8.3, 8.3 Hz), 7.31 (dd, 1H,J=8.1 Hz), 7.23 (d, 1H, J=7.4 Hz), 7.06-6.88 (m, 4H), 6.90 (m, 1H), 6.49(bs, 1H), 5.99 (bt, 1H), 5.39 (m, 2H), 4.39 (m, 2H), 3.83 (s, 3H), 3.42(q, 1H, J=7.1 Hz), 3.01 (s, 3H), 1.42 (d, 3H, J=7.1 Hz); IR (neat) 3294,1656, 1600, 1512, 1417, 1349, 1267, 1157, 976, 910, 735 cm⁻¹; MS (FAB)m/z 556 (M+H)

Example 108N-(2-butoxy-4-tert-butyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.48 (t, 1H, J=8.2 Hz), 7.16-7.04 (m, 3H),6.92-6.85 (m, 2H), 6.59 (bs, 1H), 5.98 (bt, 1H), 4.45-4.29 (m, 2H),3.98-3.90 (m, 2H), 3.46 (q, 1H, J=6.9 Hz), 3.01 (s, 3H), 1.75-1.65 (m,2H), 1.48 (d, 3H, J=7.1 Hz), 1.30 (s, 9H), 0.97 (t, 3H, J=7.3 Hz); IR(KBr) 3289, 2961, 1650, 1510, 1413, 1334 cm⁻¹; MS (FAB) m/z 479 (M+H)

Example 1092-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.54 (d, 1H, J=7.7 Hz), 7.48 (dd, 1H, J=8.2, 8.2 Hz), 7.31 (m, 3H), 7.13(dd, 1H, J=11.0, 1.8 Hz), 7.08 (d, 1H, J=8.8 Hz), 6.96-6.89 (m, 3H),6.33 (bs, 1H), 6.20 (bt, 1H), 4.54 (d, 2H, J=6.0 Hz), 3.57 (q, 1H, J=7.0Hz), 3.32-3.29 (m, 8H), 2.99 (s, 3H), 1.53 (d, 3H, J=7.1 Hz); IR (neat)3292, 1658, 1594, 1508, 1418, 1374, 1335, 1231, 1155, 968, 909, 834,758, 694 cm⁻¹; MS (FAB) m/z 580 (M+H)

Example 1102-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.67 (m, 2H), 7.59 (d, 1H, J=8.2 Hz), 7.34 (dd, 1H, J=8.2, 8.2 Hz), 7.19(dd, 1H, J=10.9, 1.9 Hz), 7.11 (d, 1H, J=8.4 Hz), 7.06 (d, 1H, J=7.7Hz), 7.02-6.95 (m, 3H), 4.45 (m, 2H), 3.67 (q, 1H, J=7.1 Hz), 2.89 (s,3H), 1.47 (d, 3H, J=7.1 Hz); IR (neat) 3306, 2926, 1706, 1645, 1509,1428, 1328, 1156, 968, 833 cm⁻¹; MS (FAB) m/z 511 (M+H)

Example 1112-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-propoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.58 (d, 1H, J=7.5 Hz), 7.52 (dd, 1H, J=8.2, 8.2 Hz),7.19 (d, 1H, J=7.3 Hz), 7.12-7.05 (m, 2H), 6.50 (bs, NH), 5.97 (bt, NH),4.39-4.23 (m, 4H), 3.52 (q, 1H, J=7.1 Hz), 3.03 (s, 3H), 1.74 (m, 2H),0.99 (t, 3H, J=7.3 Hz); IR (neat) 3287, 2972, 1655, 1513, 1426, 1336,1256, 976 cm⁻¹; MS (FAB) m/z 478 (M+H)

Example 1122-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CD₃OD)

7.90 (m, 2H), 7.59 (d, 1H, J=7.5 Hz), 7.33 (dd, 1H, J=8.3, 8.3 Hz), 7.24(m, 1H), 7.21 (dd, 1H, J=11.4, 1.8 Hz), 7.11 (d, 1H, J=8.4 Hz), 7.06 (d,1H, J=7.5 Hz), 6.59 (m, 1H), 4.46 (m, 2H), 3.68 (q, 1H, J=7.1 Hz), 2.87(s, 3H), 1.47 (d, 3H, J=7.1 Hz); IR (neat) 3267, 2928, 1707, 1644, 1593,1502, 1433, 1329, 1157, 969, 817, 755, 694 cm⁻¹; MS (FAB) m/z 529 (M+H)

Example 113N-[2-(4-chloro-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CD₃OD) δ 7.10 (d, 2H, J=9.0 Hz,) 7.62 (d, 1H, J=7.5Hz), 7.34 (dd, 1H, J=8.3, 8.3 Hz), 7.23 (d, 2H, J=9.0 Hz), 7.19 (dd, 1H,J=11.7, 2.0 Hz), 7.10 (d, 1H, J=8.3 Hz), 7.09 (d, 1H, J=7.5 Hz), 4.45(m, 2H), 3.67 (q, 1H, J=7.0 Hz), 2.88 (s, 3H), 1.47 (d, 3H, J=7.1 Hz);IR (neat) 2922, 1645, 1496, 1466, 1334, 1151, 971, 819 cm⁻¹; MS (FAB)m/z 545 (M+H)

Example 1142-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-fluoro-4-trifluoromethyl-benzyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.50 (dd, 1H, J=8.0, 8.0 Hz), 7.41-7.26 (m, 3H), 7.13 (dd, 1H, J=11.0,2.0 Hz), 7.07 (bd, 1H), 6.60 (bs, 1H), 6.00 (bt, 1H), 4.48 (m, 2H), 3.03(s, 3H), 1.49 (d, 3H J=7.1 Hz); IR (KBr) 3288, 1657, 1588, 1512, 1430,1332, 1220 cm⁻¹; MS (FAB) m/z 437 (M+H)

Example 115N-(2-benzylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.42-7.14 (m, 8H), 6.82 (d, 1H, J=7.2 Hz), 6.69 (bt, 1H), 4.68-4.44 (m,2H), 4.25 (m, 2H), 3.62 (q, 1H, J=7.1 Hz), 2.94 (s, 3H), 1.37 (d, 3H,J=7.3 Hz); IR (KBr) 3269, 2928, 2493, 1706, 1644, 1513, 1452 cm⁻¹; MS(FAB) m/z 525 (M+H)

Example 1172-(3-fluoro-4-methylsulfonamido-phenyl)-N-((2-(4-tert-butylphenyl)-6-(trifluoromethyl)pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.77 (d, 1H, J=8.1 Hz), 7.66 (d, 1H, J=8.1 Hz), 7.50 (d, 2H, J=6.6 Hz),7.40-7.45 (m, 3H), 7.06-7.19 (m, 3H), 4.40 (s, 2H), 3.65 (q, 1H, J=6.6Hz), 2.96 (s, 3H), 1.40 (d, 3H, J=6.6 Hz), 1.35 (s, 9H); IR (KBr) 2927,2856, 1619, 1511, 1455, 1339, 1274, 1158 cm⁻¹; MS (FAB) m/z 552 (M+H)

Example 1182-(3-fluoro-4-methylsulfonamido-phenyl)-(N(2-(3-chloro-4-fluorophenyl)-6-(trifluoromethyl))pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.75 (d, 1H, J=7.5 Hz), 7.63 (d, 1H, J=7.5 Hz), 7.56 (dd, 1H, J=2.1 Hz,6.9 Hz), 7.34-7.49 (m, 3H), 7.23 (t, 1H, J=7.5 Hz), 7.05-7.14 (m, 2H),4.41 (s, 2H), 3.56 (q, 1H, J=6.9 Hz), 2.98 (s, 3H), 1.40 (d, 3H, J=6.9Hz); IR (KBr) 2919, 1651, 1508, 1409, 1338, 1150, 971, 829 cm⁻¹; MS(FAB) m/z 548 (M+H)

Example 1222-(3-fluoro-4-methylsulfonamido-phenyl)-(N(2-(butylthio)-6-(trifluoromethyl)pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCJ₃)

7.42-7.50 (m, 2H), 7.27 (s, 1H), 7.13 (dd, 1H, J=8.1, 1.8 Hz), 7.07 (d,1H, J=8.1 Hz), 6.98 (bs 1H), 6.33 (bt, 1H), 4.36 (m, 2H), 3.56 (q, 1H,J=6.9 Hz), 3.22 (t, 2H, J=7.5 Hz), 3.01 (s, 3H), 1.66 (m, 2H), 1.38-1.50(m, 5H), 0.93 (t, 3H, J=7.2 Hz); IR (KBr) 3291, 2930, 2856, 1707, 1587,1513, 1337, 1272, 1154, 1108, 898, 815 cm⁻¹; MS (FAB) m/z 508 (M+H)

Example 1242-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-methyl-cyclopropylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CD₃OD)

7.48 (d, 1H, J=7.5 Hz), 7.43 (dd, 1H, J=8.1, 8.1 Hz), 7.15-7.23 (m, 3H),4.34 (d, 2H, J=5.1 Hz), 4.20 (d, 2H, J=7.1 Hz), 3.73 (q, 1H, J=6.9 Hz),2.98 (s, 3H), 1.46 (d, 3H, J=7.1 Hz), 1.04 (d, 3H, J=6.0 Hz), 0.95 (m,1H), 0.78 (m, 1H), 0.51 (m, 1H), 0.31 (m, 1H); IR (KBr) 3280, 2928,1654, 1512, 1450, 1427, 1339, 1267, 1158, 980 cm⁻¹; MS (FAB) m/z 504(M+H)

Example 1252-(3-fluoro-4-methylsulfonamido-phenyl)-(N(2-(3,3-dimethylbutoxy)-6-(trifluoromethyl)pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.40-7.48 (m, 2H), 7.13-7.22 (m, 3H), 4.42 (t, 2H, J=7.5 Hz), 4.31 (d,2H, J=7.2 Hz), 3.72 (q, 1H, J=6.9 Hz), 2.97 (s, 3H), 1.68 (t, 2H, J=7.2Hz), 1.45 (d, 3H, J=6.9 Hz), 0.97 (s, 9H); IR (KBr) 3352, 3077, 2950,1655, 1545, 1510, 1427, 1366, 1331, 1150 cm⁻¹; MS (FAB) m/z 520 (M+H)

Example 1262-(3-fluoro-4-methylsulfonamido-phenyl)-(N-(2-(cyclohexylthio)-6-(trifluoromethyl)pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.35-7.48 (m, 3H), 7.26 (d, 1H, J=7.8 Hz), 7.16 (dd, 1H, J=1.8, 11.1Hz), 7.10 (d, 1H, J=8.4 Hz), 6.13 (bs, 1H), 4.35 (d, 2H, J=5.7 Hz), 3.82(m, 1H), 3.56 (q, 1H, J=7.2 Hz), 3.02 (s, 3H), 2.06 (m, 2H), 1.75 (m,2H), 1.49 (d, 3H, J=7.2 Hz), 1.26-1.33 (m, 6H); IR (KBr) 3284, 2932,2854, 1654, 1586, 1512, 1449, 1336, 1267 cm⁻¹; MS (FAB) m/z 534 (M+H)

Example 1272-(4-methylsulfonamido-3-methyl-phenyl)-N-(6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.46 (d, 1H, J=8.1 Hz), 7.39 (d, 1H, J=8.1Hz), 7.11-7.20 (m, 3H), 6.33 (s, 1H), 6.25 (bs, 1H), 4.46 (d, 2H, J=5.7Hz), 3.56 (q, 1H, J=7.5 Hz), 2.96-3.02 (m, 7H), 2.38 (s, 3H), 1.54-1.63(m, 6H), 1.52 (d, 3H, J=7.5 Hz); IR (KBr) 3288, 2928, 2853, 1652, 1538,1457, 1246, 970 cm⁻¹; MS (FAB) m/z 499 (M+H)

Example 128N-(2-azocan-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48 (t, 1H, J=8.1 Hz), 7.36 (d, 1H, J=7.8 Hz), 7.14 (dd, 1H, J=2.1,11.1 Hz), 7.07 (d, 1H, J=8.1 Hz), 6.96 (d, 1H, J=7.8 Hz), 6.94 (bs, 1H),5.97 (bs, 1H), 4.39 (d, 2H, J=5.1 Hz), 3.59 (q, 1H, J=7.2 Hz), 3.46 (m,4H), 3.01 (s, 3H), 1.68 (m, 4H), 1.51 (m, 6H); IR (KBr) 3275, 2926,1652, 1594, 1509, 1454, 1421, 1334 cm⁻¹; MS (FAB) m/z 531 (M+H)

Example 1292-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-thiopropionamide

¹H NMR (300 MHz, CDCl₃)

7.97 (bs, 1H), 7.50 (dd, 1H, J=8.1, 8.1 Hz), 7.08-7.29 (m, 4H), 6.54(bs, 1H), 4.85 (d, 2H, J=5.7 Hz), 4.01 (q, 1H, J=6.9 Hz), 3.09 (m, 4H),3.01 (s, 3H), 1.87 (m, 4H), 1.62 (d, 3H, J=6.9 Hz); IR (KBr)) 3296,2923, 1509, 1428, 1334, 1159, 1121, 978, 907, 733 cm⁻¹; MS (FAB) m/z 505(M+H)

Example 1302-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-thiopropionamide

¹H NMR (300 MHz, CDCl₃)

7.76 (d, 1H, J=8.1 Hz), 7.60 (d, 1H, J=8.1 Hz), 7.42-7.47 (m, 3H),7.00-7.19 (m, 5H), 6.54 (bs, 1H), 4.95 (d, 2H, J=5.7 Hz), 3.93 (q, 1H,J=6.9 Hz), 3.03 (s, 3H), 1.59 (d, 3H, J=6.9 Hz); IR (KBr)) 3300, 1512,1409, 1340, 1155, 1047 cm⁻¹; MS (FAB) m/z 530 (M+H)

Example 1312-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methylpiperidin-1-yl-6-chlrorodifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.45-7.53 (m, 2H), 7.07-7.18 (m, 3H), 6.72 (bs, 1H), 6.37 (bt, 1H), 4.46(d, 2H, J=5.7 Hz), 3.56 (q, 1H, J=6.9 Hz), 3.32 (m, 2H), 3.02 (s, 3H),2.82 (m, 2H), 1.71 (m, 2H), 1.53 (d, 3H, J=7.5 Hz), 1.23 (m, 3H), 0.97(d, 3H, J=6.9 Hz); IR (KBr) 2924, 1653, 1590, 1512, 1453, 1334, 1157cm⁻¹; MS (FAB) m/z 534 (M+H)

Example 132N-[2-azepan-1-yl-6-(chloro-difluoro-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.52 (dd, 1H, J=8.1, 8.1 Hz), 7.38 (d, 1H, J=7.5 Hz), 7.17 (dd, 1H,J=1.8, 11.1 Hz), 7.08 (d, 1H, J=8.1 Hz), 6.99 (d, 1H, J=7.5 Hz), 6.57(bs, 1H), 5.87 (bt, 1H), 4.42 (d, 2H, J=5.7 Hz), 3.56 (q, 1H, J=6.9 Hz),3.39 (t, 4H, J=6.0 Hz), 3.02 (s, 3H), 1.75 (m, 4H), 1.56 (m, 4H), 1.52(d, 3H, J=6.9 Hz); IR (KBr) 3286, 2929, 1652, 1592, 1511, 1452, 1421,1333, 1159 cm⁻¹; MS (FAB) m/z 534 (M+H)

Example 1342-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.54 (dd, 1H, J=8.4, 8.4 Hz), 7.50 (d, 1H, J=8.1 Hz), 7.23 (d, 1H, J=7.7Hz), 7.14 (dd, 1H, J=11.2, 1.9 Hz), 7.09 (d, 1H, J=8.2 Hz), 6.21 (bt,1H), 4.47 (m, 2H), 3.57 (q, 1H, J=7.1 Hz), 3.19-3.15 (m, 4H), 3.04 (s,3H), 2.53-2.49 (m, 4H), 2.34 (s, 3H), 1.54 (d, 3H, J=7.1 Hz); IR (neat)2935, 1655, 1591, 1511, 1457, 1417, 1334, 1149, 966, 757 cm⁻¹; MS (FAB)m/z 518 (M+H)

Example 135N-[2-(3,4-dimethyl-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.56 (m, 2H), 7.43 (dd, 1H, J=8.4, 8.4 Hz), 7.39 (d, 1H, J=7.8 Hz), 7.14(dd, 1H, J=11.0, 2.2 Hz), 7.06 (d, 1H, J=8.7 Hz), 7.03 (d, 1H, J=7.7Hz), 6.95 (d, 1H, J=7.5 Hz), 6.41 (bs, 1H), 5.85 (bt, 1H), 4.47 (d, 2H,J=6.4 Hz), 3.52 (q, 1H, J=7.1 Hz), 2.96 (s, 3H), 2.27 (s, 3H), 2.23 (s,3H), 1.52 (d, 3H, J=7.1 Hz); IR (neat) 3363, 2922, 1646, 1538, 1509,1428, 1328, 1156, 970, 814 cm⁻¹; MS (FAB) m/z 539 (M+H)

Example 136N-[2-(5-chloro-2-methyl-phenylamino)-6-trifluoromethyl-Pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.68 (d, 1H, J=2.2 Hz), 7.45 (d, 1H, J=7.5Hz), 7.42 (dd, 1H, J=8.3, 8.3 Hz), 7.11 (d, 1H, J=7.7H), 7.08 (dd, 1H,J=9.0, 2.2 Hz), 7.03-7.00 (m, 3H), 6A3 (bs, 1H), 5.87 (bt, 1H), 4.49 (m,2H), 3.51 (q, 1H, J=7.1 Hz), 3.02 (s, 3H), 2.25 (s, 3H), 1.48 (d, 3H,J=7.1 Hz); IR (neat) 3293, 1706, 1651, 1595, 1517, 1423, 1334, 1156,969, 904, 819 cm⁻¹; MS (FAB) m/z 559 (M+H)

Example 137N-(2-azocan-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48-7.51 (m, 2H), 7.08-7.36 (m, 8H), 6.52 (s, 1H), 6.23 (bs, 1H), 4.53(d, 2H, J=5.1 Hz), 3.56 (q, 1H, J=7.2 Hz), 3.46 (m, 2H), 2.95-3.00 (m,5H), 2.03 (m, 2H), 1.82 (m, 2H), 1.54 (d, 3H, J=7.2 Hz); IR (KBr) 2933,1655, 1592, 1512, 1419, 1374, 1336, 1224, 1158, 957, 834, 758, 701 cm⁻¹;MS (FAB) m/z 579 (M+H)

Example 1382-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-fluoro-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.50 (d, 1H, J=8.1 Hz), 7.43 (t, 1H, J=8.1 Hz), 7.14-7.26 (m, 3H), 4.75(dm, 1H, J=50 Hz), 4.38 (d, 2H, J=5.7 Hz) 3.71 (q, 1H, J=7.2 Hz), 3.30(m, 2H), 3.03 (m, 2H), 2.96 (s, 3H), 1.88 (m, 4H), 1.46 (d, 3H, J=7.2Hz); IR (KBr) 2926, 2854, 1656, 1591, 1512, 1418 cm⁻¹; MS (FAB) m/z 521(M+H)

Example 1392-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47-7.52 (m, 2H), 7.06-7.22 (m, 4H), 6.68 (bs, 1H), 6.40 (bt, 1H),5.79-5.83 (m, 2H), 4.49 (d, 2H, J=5.7 Hz), 3.69 (m, 2H), 3.56 (q, 1H,J=7.2 Hz), 3.21 (m, 2H), 3.02 (s, 3H), 2.27 (m, 2H), 1.52 (d, 3H, J=7.2Hz); IR (KBr) 3286, 2924, 1654, 1592, 1512, 1423, 1337, 1271, 1158, 972,833, 737 cm⁻¹; MS (FAB) m/z 501 (M+H)

Example 1422-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.54 (d, 1H, J=7.7 Hz), 7.43 (dd, 1H, J=8.0,8.0 Hz), 7.41 (d, 1H, 7.9 Hz), 7.15 (dd, 1H, J=11.2, 1.8 Hz), 7.06 (d,1H, J=1.4 Hz), 6.20 (bt, 1H), 4.41-4.55 (m, 2H), 3.60 (q, 1H, J=7.0 Hz),3.01 (s, 3H), 2.75 (t, 2H, J=7.9 Hz), 1.61-1.71 (m, 2H), 1.51 (d, 3H,J=7.1 Hz), 1.18-1.35 (m, 4H), 0.85-0.90 (m, 3H); IR (KBr) 3289, 2930,1655, 1521, 1459, 1340, 1157, 973, 911, 732 cm⁻¹; MS (FAB) m/z 490 (M+H)

Example 147N-[2-(4-chloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.79 (d, 1H, J=8.2 Hz), 7.62 (d, 1H, J=8.1Hz), 7.53 (m, 1H), 7.37-7.45 (m, 4H), 7.06 (m, 1H), 7.02 (d, 1H, J=7.9Hz), 5.59 (bt, 1H), 4.50 (d, 2H, J=6.0 Hz), 3.48 (q, 1H, J=7.3 Hz), 3.04(s, 3H), 1.47 (d, 3H, J=7.1 Hz); IR (KBr) 3290, 1657, 1512, 1456, 1409,1339, 1154, 972, 910, 835, 732 cm⁻¹; MS (FAB) m/z 530 (M+H)

Example 1482-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.79 (d, 1H, J=8.1 Hz), 7.62 (d, 1H, J=8.1 Hz), 7.36-7.44 (m, 2H),6.97-7.19 (m, 5H), 6.90 (bs, 1H), 6.01 (bt, 1H), 4.37-4.51 (m, 2H), 3.50(q, 1H, J=7.1 Hz), 3.00 (s, 3H), 1.45 (d, 3H, J=7.1 Hz); IR (KBr) 3239,1655, 1586, 1512, 1448, 1340, 1154, 972, 912 cm⁻¹; MS (FAB) m/z 514(M+H)

Example 149N-[2-(3-chloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.82 (d, 1H, J=8.3 Hz), 7.62 (d, 1H, J=8.0 Hz), 7.52 (dd, 1H, J=8.3, 8.3Hz), 7.40-7.42 (m, 3H), 7.31 (m, 1H), 7.07 (m, 1H), 7.01 (m, 1H), 4.48(d, 2H, J=6.6 Hz), 3.48 (q, 1H, J=7.0 Hz), 3.04 (s, 3H), 1.47 (d, 3H,J=7.1 Hz); IR (KBr) 3293, 2927, 1655, 1512, 1340, 1153, 732 cm⁻¹; MS(FAB) m/z 530 (M+H)

Example 1502-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.86 (d, 1H, J=8.1 Hz), 7.66 (d, 1H, J=8.0 Hz), 7.36-7.51 (m, 3H), 7.28(m, 1H), 7.01-7.16 (m, 3H), 6.68 (bs, 1H), 5.84 (bt, 1H), 4.29-4.44 (m,2H), 3.49 (q, 1H, J=7.0 Hz), 3.02 (s, 3H), 1.47 (d, 3H, J=7.1 Hz); IR(KBr) 3292, 1658, 1512, 1340, 1156, 973, 732 cm⁻¹; MS (FAB) m/z 514(M+H)

Example 1512-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.77 (d, 1H, J=7.9 Hz), 7.57 (d, 1H, J=8.1 Hz), 7.50 (dd, 1H, J=8.3, 8.3Hz), 7.38 (d, 2H, J=8.8 Hz), 7.01-7.06 (m, 2H), 6.96 (d, 2H, J=8.9 Hz),6.50 (bs, 1H), 5.57 (bs, 1H), 4.53 (d, 2H, J=5.3 Hz), 3.86 (s, 3H), 3.46(q, 1H, J=7.0 Hz), 3.03 (s, 3H), 1.46 (d, 3H, J=7.1 Hz); IR (KBr) 2928,1655, 1514, 1340, 1251, 1155, 973, 837, 732 cm⁻¹; MS (FAB) m/z 526 (M+H)

Example 152N-[4-tert-butyl-2-(2,2-dimethyl-propoxy)-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47 (t, 1H, J=8.2 Hz), 7.16-7.11 (m, 2H), 7.04 (d, 1H, J=8.2 Hz),6.93-6.84 (m, 2H), 6.52 (bs, 1H), 5.90 (bt, 1H), 4.50-4.31 (m, 2H),3.63-3.57 (m, 2H), 3.44 (q, 1H, J=6.9 Hz), 3.01 (s, 3H), 1.47 (d, 3H,J=6.9 Hz), 1.31 (s, 9H), 1.0 (s, 9H); IR (KBr) 3292, 2960, 1649, 1511,1457, 1408 cm⁻¹; MS (FAB) m/z 493 (M+H)

Example 153N-(4-tert-butyl-2-pentyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.49 (t, 1H, J=8.2 Hz), 7.16-7.04 (m, 3H),6.92-6.85 (m, 2H) 6.52 (bs, 1H), 5.99 (bt, 1H), 4.45-4.29 (m, 2H),4.01-3.89 (m, 2H), 3.46 (q, 1H, J=7.1 Hz), 3.01 (s, 3H), 1.77-1.68 (m,2H), 1.48 (d, 3H, J=7.1 Hz), 1.43-1.39 (m, 4H), 1.30 (s, 9H), 0.93 (t,3H, J=7.1 Hz); IR (KBr) 3288, 2959, 2868, 1650, 1510, 1455 cm⁻¹; MS(FAB) m/z 493 (M+H)

Example 154N-(4-tert-butyl-2-cyclohexyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.50 (t, 1H, J=8.4 Hz), 7.17-6.86 (m, 5H),6.44 (bs, 1H), 6.01 (bt, 1H), 4.45-4.30 (m, 3H), 3.47 (q, 1H, J=6.9 Hz),3.01 (s, 3H), 1.95-1.25 (m, 10H), 1.48 (d, 3H, J=7.1 Hz), 1.29 (s, 9H);IR (KBr) 3292, 2935, 2859, 1650, 1509, 1454 cm⁻¹; MS (FAB) m/z 505 (M+H)

Example 155N-(4-tert-butyl-2-cyclopentyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.49 (t, 1H, J=8.2 Hz), 7.16-7.04 (m, 3H),6.90-6.86 (m, 2H), 6.51 (bs, 1H), 5.94 (bt, 1H), 4.78-4.76 (m, 1H),4.41-4.25 (m, 2H), 3.46 (q, 1H, J=7.1 Hz), 3.01 (s, 3H), 1.90-1.61 (m,8H), 1.48 (d, 3H, J=7.1 Hz), 1.29 (s, 9H); IR (KBr) 3289, 2962, 2870,1650, 1509, 1411 cm⁻¹; MS (FAB) m/z 491 (M+H)

Example 156N-(2-cyclobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.58-7.51 (m, 2H), 7.18 (d, 1H, J=7.3 Hz), 7.13-7.07(m, 2H), 6.50 (bs, NH), 6.00 (bt, NH), 5.20 (m, 1H), 4.37 (d, 2H, J=6.2Hz), 3.56 (q, 1H, J=7.0 Hz), 3.03 (s, 3H), 2.50-2.40 (m, 2H), 2.05-1.65(m, 4H), 1.50 (d, 3H, J=7.1 Hz); IR (neat) 3290, 2987, 1655, 1513, 1421,1340, 1275, 1157, 1071, 962 cm⁻¹; MS (FAB) m/z 490 (M+H)

Example 1572-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (CDCl₃) δ 7.57-7.49 (m, 2H), 7.16 (d, 1H, J=7.3 Hz), 7.12-7.05(m, 2H), 6.48 (bs, NH), 5.99 (bt, NH), 5.00 (m, 1H), 4.34 (d, 2H, J=5.8Hz), 3.51 (q, 1H, J=6.8 Hz), 3.03 (s, 3H), 2.12-2.00 (m, 2H), 1.80-1.72(m, 2H), 1.50-1.10 (m, 5H), 1.48 (d, 3H, J=7.1 Hz), 0.94 (d, 3H, J=6.6Hz); IR (neat) 3287, 2931, 1655, 1513, 1422, 1336, 1271, 1158, 914, 734cm⁻¹; MS (FAB) m/z 532 (M+H)

Example 158 acetic acid3′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-ylester

¹H NMR (CDCl₃) δ 7.57-7.48 (m, 2H), 7.24 (d, 1H, J=8.1 Hz), 7.17-7.09(m, 2H), 6.47 (bs, NH), 6.05 (bt, NH), 4.93 (m, 1H), 4.47 (d, 2H, J=5.7Hz), 3.57 (q, 1H, J=7.0 Hz), 3.35-3.25 (m, 2H), 3.07-2.97 (m, 2H), 3.04(s, 3H), 2.08 (s, 3H), 2.02-1.92 (m, 2H), 1.80-1.70 (m, 2H), 1.54 (d,3H, J=7.3 Hz); IR (neat) 3362, 2910, 1726, 1657, 1512, 1419, 1335, 1260,1157, 1033, 758 cm⁻¹; MS (FAB) m/z 561 (M+H)

Example 1592-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.53-7.47 (m, 2H), 7.22 (d, 1H, J=7.7 Hz), 7.15-7.07(m, 2H), 6.77 (bs, NH), 6.32 (bt, NH), 4.47 (d, 2H, J=5.7 Hz), 3.58 (q,1H, J=7.1 Hz), 3.40-3.25 (m, 3H), 3.37 (s, 3H), 3.03 (s, 3H), 2.95-2.86(m, 2H), 2.04-1.95 (m, 2H), 1.63-1.50 (m, 2H), 1.53 (d, 3H, J=7.0 Hz);IR (neat) 3289, 2932, 1656, 1592, 1512, 1457, 1418, 1335, 1275, 1158,733 cm⁻¹; MS (FAB) m/z 533 (M+H)

Example 160N-(4-butoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)propionamide

¹H NMR (CDCl₃) δ 7.54-7.48 (m, 2H), 7.21 (d, 1H, J=7.5 Hz), 7.14-7.07(m, 2H), 6.64 (bs, NH), 6.26 (bt, NH), 4.47 (d, 2H, J=5.7 Hz), 3.57 (q,1H, J=7.1 Hz), 3.50-3.26 (m, 5H), 3.03 (s, 3H), 2.94-2.86 (m, 2H),2.02-1.95 (m, 2H), 1.62-1.50 (m, 7H), 1.45-1.33 (m, 2H), 0.93 (t, 3H,J=7.3 Hz); IR (neat) 3295, 2931, 1654, 1513, 1458, 1420, 1335, 1157cm⁻¹; MS (FAB) m/z 575 (M+H)

Example 161N-(2-cyclopentylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.58 (d, 1H, J=7.3 Hz), 7.51 (dd, 1H, J=8.4, 8.4 Hz),7.19 (d, 1H, J=7.3 Hz), 7.11-7.04 (m, 2H), 6.54 (bs, NH), 6.00 (bt, NH),4.38 (m, 2H), 4.20 (m, 2H), 3.50 (q, 1H, J=7.1 Hz), 3.03 (s, 3H), 2.29(m, 1H), 1.80-1.70 (m, 2H), 1.70-1.55 (m, 4H), 1.48 (d, 3H, J=7.1 Hz),1.37-1.27 (m, 2H); IR (neat) 3293, 2952, 1655, 1513, 1424, 1338, 1158cm⁻¹; MS (FAB) m/z 518 (M+H)

Example 1622-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-isopropoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.55-7.48 (m, 2H), 7.22 (d, 1H, J=7.7 Hz), 7.15-7.08(m, 2H), 6.56 (bs, NH), 6.23 (bt, NH), 4.47 (d, 2H, J=5.9 Hz), 3.74 (m,1H), 3.60-3.45 (m, 2H), 3.37-3.33 (m, 2H), 3.04 (s, 3H), 2.94-2.85 (m,2H), 1.98-1.90 (m, 2H), 1.62-1.50 (m, 2H), 1.53 (d, 3H, J=7.0 Hz), 1.18(d, 6H, J=6.1 Hz); IR (neat) 3289, 2925, 1655, 1593, 1513, 1335, 1155cm⁻¹; MS (FAB) m/z 561 (M+H)

Example 163N-(2-ethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.58 (d, 1H, J=7.3 Hz), 7.51 (dd, 1H, J=8.2, 8.2 Hz),7.19 (d, 1H, J=7.3 Hz), 7.12-7.05 (m, 2H), 6.58 (bs, NH), 6.02 (bt, NH),4.44-4.36 (m, 4H), 3.53 (q, 1H, J=7.0 Hz), 3.03 (s, 3H), 1.49 (d, 3H,J=7.1 Hz), 1.34 (t, 3H, J=7.1 Hz); IR (neat) 3294, 1654, 1513, 1425,1342, 1156 cm⁻¹; MS (FAB) m/z 464 (M+H)

Example 1642-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6″-trifluoromethyl-3,4,5,6,3′,4′,5′,6′-octahydro-2H,2′H-[1,4′;1′,2″]terpyridin-3″-ylmethyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.51 (d, 1H, J=7.7 Hz), 7.42 (dd, 1H, J=8.2, 8.2 Hz), 7.53 (d, 1H, J=7.7Hz), 7.13-7.21 (m, 2H), 4.30-4.47 (m, 2H), 3.71 (q, 1H, J=7.0 Hz),3.48-3.52 (m, 2H), 2.97 (s, 3H), 2.80-2.84 (m, 2H), 2.55-2.75 (m, 5H),1.88-2.00 (m, 2H), 1.60-1.75 (m, 6H), 1.50-1.55 (m, 2H), 1.46 (d, 3H,J=7.0 Hz); IR (KBr) 2924, 1649, 1509, 1456, 1419, 1334, 1124, 961 cm⁻¹;MS (FAB) m/z 586 (M+H)

Example 1652-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-pyrrolidin-1-yl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)propionamide

¹H NMR (300 MHz, CD₃OD)

7.50 (d, 1H, J=7.7 Hz), 7.42 (dd, 1H, J=8.3, 8.3 Hz), 7.25 (d, 1H, J=7.7Hz), 7.10-7.22 (m, 2H), 4.29-4.45 (m, 2H), 3.72 (q, 1H, J=7.1 Hz),3.40-3.50 (m, 2H), 2.70-2.92 (m, 6H), 2.40 (m, 1H), 1.95-2.10 (m, 2H),1.81-2.10 (m, 4H), 1.57-1.74 (m, 2H), 1.46 (d, 3H, J=7.0 Hz)

IR (KBr) 3296, 2926, 1651, 1580, 1420, 1333, 1126, 980, 832 cm⁻¹; MS(FAB) m/z 572 (M+H)

Example 166N-[6-(chloro-difluoro-methyl)-2-cyclopentyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48-7.57 (m, 2H), 7.03-7.15 (m, 3H), 6.56 (bs, 1H), 5.96 (bt, 1H), 5.46(m, 1H), 4.27-4.42 (m, 2H), 3.52 (q, 1H, J=7.1 Hz), 3.03 (s, 3H),1.19-2.08 (m, 2H), 1.56-1.78 (m, 6H), 1.49 (d, 3H, J=7.1 Hz);

IR (KBr) 3288, 2967, 1655, 1512, 1419, 1339, 1159, 1112, 989, 889 cm⁻¹;MS (FAB) m/z 520 (M+H)

Example 167N-[2-(butyl-methyl-amino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.53 (dd, 1H, J=8.3, 8.3 Hz), 7.45 (d, 1H, J=7.9 Hz), 7.05-7.19 (m, 3H),6.52 (bs, 1H), 6.13 (bt, 1H), 4.46 (d, 2H, J=5.9 Hz), 3.56 (q, 1H, J=7.1Hz), 3.05-3.12 (m, 2H), 3.04 (s, 3H), 2.80 (s, 3H), 1.42-1.58 (m, 5H),1.20-1.38 (m, 2H), 0.90 (t, 3H, J=7.3 Hz); IR (KBr) 3280, 2932, 1653,1511, 1460, 1400, 1335, 1159, 971 cm⁻¹; MS (FAB) m/z 505 (M+H)

Example 168N-[6-(chloro-difluoro-methyl)-2-cyclohexyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ

7.48-7.59 (m, 2H), 7.02-7.14 (m, 3H), 6.49 (bs, 1H), 6.01 (bt, 1H), 5.13(m, 1H), 4.29-4.47 (m, 2H), 3.52 (q, 1H, J=7.3 Hz), 3.03 (s, 3H),1.85-1.99 (m, 2H), 1.62-1.77 (m, 2H), 1.38-1.52 (m, 9H); IR (KBr) 3288,2935, 2857, 1653, 1512, 1420, 1335, 1266, 1158, 1114, 987, 882 cm⁻¹; MS(FAB) m/z 534 (M+H)

Example 169N-[2-benzyloxy-6-(chloro-difluoro-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.59 (d, 1H, J=7.3 Hz), 7.30-7.50 (m, 6H), 7.20 (d, 1H, J=7.8 Hz), 7.05(dd, 1H, J=11.2, 2.0 Hz), 6.97 (d, 1H, J=7.9 Hz), 6.52 (bs, 1H), 6.00(bt, 1H), 5.36-5.49 (m, 2H), 4.30-4.46 (m, 2H), 3.42 (q, 1H, J=7.1 Hz),3.00 (s, 3H), 1.43 (d, 3H, J=7.1 Hz); IR (KBr) 3286, 1653, 1511, 1417,1334, 1267, 1157, 1114, 971, 883, 756 cm⁻¹; MS (FAB) m/z 542 (M+H)

Example 170N-[2-(4-tert-butyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.57-7.50 (m, 2H), 7.16 (d, 1H, J=7.3 Hz), 7.12-7.05(m, 2H), 6.46 (bs, NH), 5.98 (bt, NH), 4.96 (m, 1H), 4.34 (m, 2H), 3.51(q, 1H, J=7.1 Hz), 3.03 (s, 3H), 2.20-2.10 (m, 2H), 1.88-1.80 (m, 2H),1.49 (d, 3H, J=7.1 Hz), 1.30-1.00 (m, 5H), 0.89 (s, 9H); IR (neat) 3291,2950, 2866, 1654, 1513, 1422, 1338, 1268, 1158 cm⁻¹; MS (FAB) m/z 574(M+H)

Example 171N-[2-(4-ethyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.57-7.50 (m, 2H), 7.16 (d, 1H, J=7.3 Hz), 7.12-7.05(m, 2H), 6.47 (bs, NH), 5.99 (bt, NH), 5.00 (m, 1H), 4.34 (m, 2H), 3.52(q, 1H, J=7.5 Hz), 3.03 (s, 3H), 2.13-2.03 (m, 2H), 1.87-1.80 (m, 2H),1.49 (d, 3H, J=7.1 Hz), 1.32-1.04 (m, 7H), 0.91 (t, 3H, J=7.1 Hz); IR(neat) 3287, 2935, 2858, 1655, 1513, 1421, 1337, 1269, 1159 cm⁻¹; MS(FAB) m/z 546 (M+H)

Example 1722-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.61 (d, 1H, J=7.4 Hz), 7.47 (dd, 1H, J=8.1, 8.1 Hz), 7.31 (d, 2H, J=8.0Hz), 7.22 (d, 1H, J=7.2 Hz), 7.20 (d, 2H, J=7.9 Hz), 7.03 (dd, 1H,J=11.5, 1.9 Hz), 6.96 (d, 1H, J=8.6 Hz), 6.46 (bs, 1H), 5.98 (bt, 1H),5.36 (m, 2H), 4.37 (m, 2H), 3.40 (q, 1H, J=7.1 Hz), 3.01 (s, 3H), 2.28(s, 3H), 1.42 (d, 3H, J=7.0 Hz); IR (neat) 3289, 2925, 1654, 1513, 1458,1422, 1137, 1267, 1158, 976, 933, 808 cm⁻¹; MS (FAB) m/z 540 (M+H)

Example 173N-[2-(4-chloro-benzylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.48 (dd, 1H, J=8.3, 8.3 Hz), 7.33 (d, 2H,J=8.6 Hz), 7.25 (d, 2H, J=8.6 Hz), 7.24 (d, 1H, J=7.5 Hz), 7.07 (dd, 1H,J=11.2, 2.0 Hz), 6.99 (d, 1H, J=8.4 Hz), 6.81 (d, 1H, J=7.5 Hz), 6.71(bt, 1H), 6.47 (bs, 1H), 5.72 (bs, 1H), 4.58 (m, 2H), 4.32 (m, 2H), 3.44(q, 1H, J=7.1 Hz), 3.03 (s, 3H), 1.42 (d, 3H, J=7.1 Hz); IR (neat) 3343,2929, 1706, 16347, 1610, 1514, 1454, 1334, 1158, 1016, 973, 909, 833,760 cm⁻¹; MS (FAB) m/z 559 (M+H)

Example 174N-(2-azepan-1-yl-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.51 (dd, 1H, J=8.2, 8.2 Hz), 7.32 (s, 1H), 7.23 (s, 2H), 7.14 (dd, 1H,J=11.3, 1.9 Hz), 7.08 (d, 1H, J=8.2 Hz), 6.52 (bs, 1H), 6.43 (bt, 1H),4.53 (m, 2H), 3.54 (q, 1H, J=7.0 Hz), 3.04-3.00 (m, 7H), 1.72-1.64 (m,8H), 1.52 (d, 3H, J=7.0 Hz); IR (neat) 3273. 2930, 2854, 1650, 1510,1424, 1335, 1159, 1121, 972, 901, 737 cm⁻¹; MS (FAB) m/z 516 (M+H)

Example 175N-[2-(4-fluoro-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.59 (d, 1H, J=7.3 Hz), 7.48 (dd, 1H, J=8.3, 8.3 Hz) 7.41 (m, 2H), 7.23(d, 1H, J=7.5 Hz), 7.06 (m, 3H), 6.99 (d, 1H, J=8.0 Hz), 6.51 (bs, 1H),5.93 (bt, 1H), 5.37 (m, 2H), 4.38 (m, 2H), 3.45 (q, 1H, J=7.1 Hz), 3.02(s, 3H), 1.44 (d, 3H, J=7.1 Hz); IR (neat) 2925, 1654, 1603, 1512, 1423,1337, 1268, 1225, 1158, 975, 931, 759 cm⁻¹; MS (FAB) m/z 544 (M+H)

Example 1762-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-pyridin-4-yl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

8.28 (d, 2H, J=6.4 Hz), 7.55 (d, 1H, J=7.9 Hz), 7.50 (dd, 1H, J=8.2, 8.2Hz), 7.29 (d, 1H, J=7.9 Hz), 7.14 (dd, 1H, J=11.4, 2.0 Hz), 7.09 (d, 1H,J=8.3 Hz), 6.69 (d, 2H, J=6.6 Hz), 6.26 (bt, 1H), 4.52 (d, 2H, J=5.7Hz), 3.60 (q, 1H, J=7.0 Hz), 3.43-3.38 (m, 4H), 3.29-3.25 (m, 4H), 3.02(s, 3H), 1.54 (d, 3H, J=7.1 Hz); IR (neat) 2848, 1650, 1597, 1512, 1454,1416, 1333, 1238, 1152, 994, 966, 808, 735 cm⁻¹; MS (FAB) m/z 581 (M+H)

Example 1772-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-4-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

8.49 (d, 2H, J=6.2 Hz), 7.61 (d, 1H, J=7.4 Hz), 7.49 (d, 2H, J=6.2 Hz),7.40 (dd, 1H, J=8.3, 8.3 Hz), 7.32 (d, 1H, J=7.4 Hz), 7.19 (dd, 1H,J=11.5, 2.0 Hz), 7.14 (d, 1H, J=8.4 Hz), 5.49 (s, 2H), 4.35 (m, 2H),3.72 (q, 1H, J=6.9 Hz), 2.96 (s, 3H), 1.45 (d, 3H, J=7.0 Hz);

IR (neat) 3735, 3264, 1640, 1514, 1462, 1419, 1335, 1270 1154, 970, 827cm⁻¹; MS (FAB) m/z 527 (M+H)

Example 1782-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenethyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.60 (d, 1H, J=7.4 Hz), 7.46 (dd, 1H, J=8.3, 8.3 Hz), 7.33 (m, 5H), 7.19(d, 1H, J=7.3 Hz), 6.97 (dd, 1H, J=11.3, 1.8 Hz), 6.89 (d, 1H, J=8.9Hz), 6.43 (bs, 1H), 5.70 (bt, 1H), 4.66 (m, 1H), 4.50 (m, 1H), 4.28 (d,2H, J=6.2 Hz), 3.14-3.05 (m, 3H), 2.99 (s, 3H), 1.36 (d, 3H, J=7.1 Hz);IR (neat) 3296, 2925, 1659, 1602, 1511, 1424, 1337, 1269, 1158, 973,755, 701 cm⁻¹; MS (FAB)) m/z 539 (M+H)

Example 1792-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide

¹H NMR (300 MHz, CDCl₃)

7.53 (d, 1H, J=7.5 Hz), 7.49 (dd, 1H, J=7.9, 7.9 Hz), 7.27 (d, 1H, J=7.5Hz), 7.14 (d, 1H, J=11.0 Hz), 7.08 (d, 1H, J=8.4 Hz), 6.99 (m, 2H), 6.90(m, 2H), 6.58 (bs, 1H), 6.17 (bt, 1H), 4.52 (d, 2H, J=5.7 Hz), 3.58 (q,1H, J=6.8 Hz), 3.29-3.25 (m, 4H), 3.22-3.18 (m, 4H), 3.01 (s, 3H), 1.53(d, 3H, J=7.1 Hz); IR (neat) 3296, 2925, 2851, 1658, 1591, 1510, 1418,1335, 1232, 1156, 968, 828, 758 cm⁻¹; MS (FAB) m/z 598 (M+H)

Example 180N-[6-(chloro-difluoro-methyl)-2-hexyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (400 MHz, CDCl₃)

7.47-7.58 (m, 2H), 7.03-7.17 (m, 3H), 6.50 (bs, 1H), 5.98 (bt, 1H),4.25-4.43 (m, 4H), 3.51 (q, 1H, J=6.8 Hz), 3.03 (s, 3H), 1.67-1.78 (m,2H), 1.49 (d, 3H, J=6.8 Hz), 1.27-1.46 (m, 6H), 0.87-0.94 (m, 3H); IR(KBr) 3291, 2930, 1654, 1512, 1424, 1337, 1267, 1158, 1113, 974, 880cm⁻¹; MS (FAB) m/z 536 (M+H)

Example 181N-[6-(chloro-difluoro-methyl)-2-(pyridin-3-ylmethoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (400 MHz, CDCl₃) δ 8.56-8.61 (m, 2H), 7.77 (m, 1H), 7.62 (d, 1H,J=7.6 Hz), 7.48 (dd, 1H, J=8.0, 8.0 Hz), 7.31 (m, 1H), 7.21 (d, 1H,J=7.6 Hz), 6.92-7.09 (m, 2H), 5.88 (bt, 1H), 5.37-5.47 (m, 2H),4.30-4.43 (m, 2H), 3.49 (q, 1H J=6.8 Hz), 3.03 (s, 3H), 1.28 (d, 3H,J=6.8 Hz); IR (KBr) 2964, 1656, 1597, 1511, 1414, 1332, 1262, 1155,1094, 1020, 800, 732 cm⁻¹; MS (FAB) m/z 543 (M+H)

Example 182N-[6-(chloro-difluoro-methyl)-2-(pyridin-2-ylmethoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (400 MHz, CDCl₃) δ 8.62 (d, 1H, J=4.4 Hz), 7.75 (dd, 1H, J=7.6,7.6 Hz), 7.67 (d, 1H, J=7.2 Hz), 7.40-7.51 (m, 2H), 7.19-7.27 (m, 2H),7.13 (dd, 1H, J=11.2, 1.6 Hz), 7.04 (d, 1H, J=8.4 Hz), 6.50 (bs, 1H),5.48-5.63 (m, 2H), 4.40-4.61 (m, 2H), 3.60 (q, 1H, J=7.2 Hz), 3.05 (s,3H), 1.49 (d, 3H, J=7.2 Hz); IR (KBr) 3287, 1659, 1596, 1511, 1454,1415, 1334, 1270, 1157, 1117, 971, 882, 828, 758 cm⁻¹; MS (FAB) m/z 543(M+H)

Example 183N-(2-dibutylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.51-7.43 (m, 2H), 7.19-7.07 (m, 3H), 6.96 (bs, 1H), 6.40 (bt, 1H), 4.50(m, 2H), 3.56 (q, 1H, J=7.1 Hz), 3.13 (m, 4H), 3.02 (s, 3H), 1.52 (d,3H, J=7.1 Hz) 1.50 (m, 4H), 1.31-1.10 (m, 4H), 0.87 (t, 6H, J=7.1 Hz);IR (KBr) 3294, 2960, 1655, 1593, 1513, 1462, 1419 cm⁻¹; MS (FAB) m/z 547(M+H)

Example 1842-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6′-(4-fluoro-phenyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.49-7.54 (m, 2H), 7.51 (dd, 1H, J=8.1, 8.1 Hz), 7.43 (d, 1H, 7.8 Hz),7.29 (d, 1H, J=7.8 Hz), 7.09-7.17 (m, 4H), 6.64 (bt, 1H), 4.48 (d, 2H,J=5.7 Hz), 3.52 (q, 1H, J=6.9 Hz), 3.30 (m, 2H), 3.03 (s, 3H), 2.88 (m,2H), 1.76 (m, 2H), 1.51 (d, 3H, J=6.9 Hz), 1.24 (m, 3H), 0.99 (d, 3H,J=6.6 Hz); IR (KBr) 3292, 2962, 1653, 1512, 1457, 1423, 1335, 1267,1158, 1113, 977, 889, 824 cm⁻¹; MS (FAB) m/z 508 (M+H)

Example 1852-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6′-(4-fluoro-phenyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.95-8.00 (m, 2H), 7.52 (dd, 1H, J=8.1, 8.1 Hz), 7.37 (d, 1H J=7.5 Hz),7.08-7.18 (m, 5H), 6.43 (bs, 1H), 6.07 (bt, 1H), 4.44 (d, 2H, J=5.7 Hz),3.54 (q, 1H, J=7.2 Hz), 3.40 (m, 2H), 3.00 (s, 3H), 1.78 (m, 4H), 1.61(m, 4H), 1.52 (d, 3H, J=7.2 Hz); IR (KBr) 3287, 2927, 1649, 1509, 1448,1333, 1228, 1157, 972, 909, 813, 732 cm⁻¹; MS (FAB) m/z 508 (M+H)

Example 186N-[6-(chloro-difluoro-methyl)-2-dipropylamino-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.53 (dd, 1H, J=8.1, 8.1 Hz), 7.43 (d, 1H, J=7.8 Hz), 7.16 (dd, 1H,J=2.1, 10.8 Hz), 7.08-7.12 (m, 2H), 6.46 (bs, 1H), 6.15 (bt, 1H), 4.44(d, 2H, J=5.7 Hz), 3.53 (q, 1H, J=6.9 Hz), 3.10 (m, 4H), 3.02 (s, 3H),1.44-1.54 (m, 4H), 0.83 (t, 6H, J=7.2 Hz); IR (KBr) 3288, 2965, 1652,1591, 1511, 1456, 1419, 1334, 1158, 1110, 974, 938, 820, 734 cm⁻¹; MS(FAB) m/z 535 (M+H)

Example 187N-[6′-(chloro-difluoro-methyl)-3,5-dimethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.45-7.54 (m, 2H), 7.06-7.15 (m, 3H), 6.62 (bs, 1H), 6.31 (bt, 1H), 4.46(d, 2H, J=5.7 Hz), 3.54 (q, 1H, J=7.2 Hz), 3.25 (m, 2H), 3.02 (s, 3H),2.36 (m, 2H), 2.03 (m, 1H), 1.53-1.65 (m, 3H), 1.52 (d, 3H, J=7.2 Hz)0.92 (d, 3H, J=6.6 Hz), 0.88 (d, 3H, J=6.6 Hz); IR (neat) 2926, 1653,1591, 1511, 145, 1334, 1253, 1017, 967, 733 cm⁻¹; MS (FAB) m/z 548 (M+H)

Example 188N-[2-(1,3-dihydro-isoindol-2-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.46 (d, 1H, J=7.5 Hz), 7.25-7.37 (m, 5H), 7.01-7.10 (m, 3H), 6.24 (bs,1H), 5.75 (bt, 1H), 4.84 (s, 4H), 4.59 (d, 2H, J=5.7 Hz), 3.52 (q, 1H,J=7.2 Hz), 2.94 (s, 3H), 1.49 (d, 3H, J=7.2 Hz); IR (KBr) 3298, 2922,1650, 1512, 1457, 1425, 1334, 1155, 747 cm⁻¹; MS (FAB) m/z 537 (M+H)

Example 1893′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-carbonicacid ethyl ester

¹H NMR (300 MHz, CDCl₃)

7.28-7.50 (m, 7H), 7.21 (d, 1H, 7.8 Hz), 7.12 (dd, 1H, J=7.8, 2.1 Hz),7.04 (d, 1H, J=8.1 Hz), 6.44 (bs, 1H), 6.13 (bt, 1H), 4.47 (d, 2H, J=5.7Hz), 4.14 (q, 2H, J=7.2 Hz), 3.52 (q, 1H, J=6.9 Hz), 3.37 (m, 2H),2.98-3.05 (m, 5H), 2.66 (m, 2H), 1.99 (m, 2H), 1.52 (d, 3H, J=7.2 Hz),1.18 (t, 3H, 6.9 Hz); IR (neat) 2927, 1721, 1654, 1512, 1455, 1336,1159, 968 cm⁻¹; MS (FAB) m/z 651 (M+H)

Example 190N-(4,6′-bis-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47-7.51 (m, 2H), 7.25 (d, 1H, J=7.8 Hz), 7.08-7.15 (m, 2H), 6.34 (bs1H), 6.04 (bt, 1H), 4.47 (d, 2H, J=5.7 Hz), 3.61 (q, 1H, J=6.9 Hz), 3.43(m, 2H), 3.01 (s, 3H), 2.84 (t, 2H, J=11.1 Hz), 1.95 (m, 2H), 1.66 (m,1H), 1.53 (d, 3H, J=6.9 Hz); IR (KBr) 2934, 1655, 1591, 1512, 1420,1337, 1255, 1146, 1083, 960, 908 cm⁻¹; MS (FAB) m/z 571 (M+H)

Example 195N-(4,6′-bis-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48 (d, 1H, J=7.8 Hz), 7.38 (d, 1H, J=8.1 Hz), 7.23 (d, 1H, J=7.8 Hz),7.11-7.15 (m, 2H), 6.60 (bs, 1H), 6.12 (bt, 1H), 4.45 (d, 2H, J=5.7 Hz),3.58 (q, 1H, J=6.9 Hz), 3.40 (m, 2H), 3.01 (s, 3H), 2.80 (m, 2H), 2.30(s, 3H), 2.19 (m 1H), 1.94 (m, 2H), 1.62 (m, 2H), 1.52 (d, 3H, J=6.9Hz); IR (KBr) 2929, 1655, 1504, 1420, 1335, 1254, 1147, 1083, 959 cm⁻¹;MS (FAB) m/z 567 (M+H)

Example 1962-(4-methylsulfonamido-3-methyl-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.46 (d, 1H, J=7.5 Hz), 7.39 (d, 1H, J=7.8 Hz), 7.18 (d, 1H, J=7.8 Hz),7.11-7.14 (m, 2H), 6.37 (bs, 1H), 6.21 (bt, 1H), 4.45 (d, 2H, J=5.7 Hz),3.56 (q, 1H, J=6.9 Hz), 3.29 (m, 2H), 3.01 (s, 3H), 2.79 (m, 2H), 2.29(s, 3H), 2.19 (m 1H), 2.05 (m, 2H), 1.69 (m, 2H), 1.52 (d, 3H, J=6.9Hz); IR (KBr) 3290, 2926, 1654, 1593, 1503, 1457, 1419, 1374, 1328,1152, 970, 732 cm⁻¹; MS (FAB) m/z 513 (M+H)

Example 197N-(4-ethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.47-7.52 (m, 2H), 7.19 (d, 1H, J=7.8 Hz), 7.06-7.14 (m, 2H), 6.69 (bs,1H), 6.37 (bt, 1H), 4.47 (d, 2H, J=5.7 Hz), 3.56 (q, 1H, J=6.9 Hz), 3.33(m, 2H), 3.02 (s, 3H), 2.80 (m, 2H), 1.76 (m, 2H), 1.52 (d, 3H, J=6.9Hz), 1.21-1.32 (m, 5H), 0.91 (t, 3H, J=7.2 Hz); IR (KBr) 3288, 2929,1655, 1591, 1512, 1419, 1336, 1275, 1158, 956, 910, 733 cm⁻¹; MS (FAB)m/z 531 (M+H)

Example 1982-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

7.75 (d, 1H, J=7.2 Hz), 7.00-7.49 (m, 9H, J=7.8 Hz), 6.26 (bt, 1H), 4.51(d, 2H, J=5.7 Hz), 3.56 (q, 1H, J=6.9 Hz), 3.01 (s, 3H), 1.48 (d, 3H,J=6.9 Hz); IR (KBr) 3291, 2927, 1659, 1589, 1513, 1406, 1335, 1260,1156, 972, 940, 835, 757 cm⁻¹; MS (FAB) m/z 512 (M+H)

Example 1992-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methoxymethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.46-7.52 (m, 2H), 7.20 (d, 1H, J=7.8 Hz), 7.07-7.15 (m, 2H), 6.82 (bs,1H), 6.37 (bt, 1H), 4.46 (d, 2H, J=5.7 Hz), 3.58 (q, 1H, J=6.9 Hz),3.26-3.38 (m, 5H), 3.02 (s, 3H), 2.82 (m, 2H), 1.79 (m, 3H), 1.51 (d,3H, J=6.9 Hz), 1.25-1.30 (m, 4H); IR (KBr) 3289, 2927, 1657, 1592, 1512,1455, 1420, 1375, 1335, 1275, 1157, 971, 832, 753 cm⁻¹; MS (FAB) m/z 547(M+H)

Example 2002-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.46-7.51 (m, 2H), 6.97-7.25 (m, 7H), 6.72 (bs 1H), 6.24 (bt, 1H), 4.50(d, 2H, J=5.7 Hz), 3.59 (q, 1H, J=6.9 Hz), 3.45 (m, 2H), 3.00 (s, 3H),2.93 (m, 2H), 1.92 (m, 2H), 1.76 (m, 3H), 1.51 (d, 3H, J=6.9 Hz); IR(KBr) 2927, 1653, 1511, 1455, 1420, 1336, 1224, 1159, 959, 833, 732cm⁻¹; MS (FAB) m/z 597 (M+H)

Example 2012-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide

¹H NMR (300 MHz, CDCl₃)

7.53 (d, 1H, J=8.1 Hz), 7.52 (dd, 1H, J=8.3, 8.3 Hz), 7.27 (d, 1H, J=8.0Hz), 7.11 (m, 4H), 6.98 (m, 2H), 6.40 (bs, 1H), 6.16 (bt, 1H), 4.53 (d,2H, J=4.6 Hz), 3.58 (q, 1H, J=7.3 Hz), 3.32-3.28 (m, 4H), 3.18-3.15 (m,4H), 3.01 (s, 3H), 1.54 (d, 3H, J=7.0 Hz); IR (neat) 2391, 2846, 1707,1657, 1591, 1504, 1453, 1417, 1336, 1235, 1157, 968, 835, 757 cm⁻¹; MS(FAB) m/z 598 (M+H)

Example 2022-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-2-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

8.61 (d, 1H, J=4.7 Hz), 7.74 (dd, 1H, J=7.6, 1.7 Hz), 7.67 (d, 1H, J=7.3Hz), 7.42 (dd, 1H, J=8.2, 8.2 Hz), 7.43 (d, 1H, J=7.7 Hz), 7.33 (m, 1H),7.24 (d, 1H, J=7.5 Hz), 7.09 (dd, 1H, J=11.4, 2.0 Hz), 7.01 (d, 1H,J=8.2 Hz), 6.54 (bs, 1H), 5.51 (m, 2H), 4.45 (d, 2H, J=5.7 Hz), 3.58 (q,1H, J=7.0 Hz), 3.01 (s, 3H), 1.46 (d, 3H, J=7.0 Hz); IR (neat) 3271,1656, 1598, 1512, 1417, 1335, 1273, 1155, 973, 935, 835, 761 cm⁻¹; MS(FAB) m/z 527 (M+H)

Example 2032-(4-methylsulfonamido-3-methyl-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.53 (d, 1H, J=7.7 Hz), 7.32 (m, 4H), 7.14 (s,1H), 7.13 (d, 1H, J=7.0 Hz), 6.92 (m, 3H), 6.18 (bt, 1H), 5.89 (bs, 1H),4.53 (d, 2H, J=5.7 Hz), 3.56 (q, 1H, J=7.1 Hz), 3.27-3.15 (m, 8H), 2.98(s, 3H), 2.23 (s, 3H), 1.51 (d, 3H, J=7.1 Hz); IR (neat) 2920, 1652,1596, 1503, 1418, 1331, 1231, 1150, 967, 761 cm⁻¹; MS (FAB) m/z 576(M+H)

Example 204N-(2-benzyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.60 (d, 1H, J=7.5 Hz), 7.39-7.33 (m, 6H),7.22 (d, 1H, J=7.3 Hz), 7.05 (s, 1H), 7.04 (d, 1H, J=7.5 Hz), 6.10 (bs,1H), 5.91 (bt, 1H), 5.37 (q, 2H, J=12.5 Hz), 4.37 (d, 2H, J=6.1 Hz),3.43 (q, 1H, J=7.1 Hz), 3.00 (s, 3H), 2.24 (s, 3H), 1.43 (d, 3H, J=7.1Hz); IR (neat) 3295, 2925, 1655, 1505, 1459, 1420, 1356, 1326, 1151,977, 756 cm⁻¹; MS (FAB) m/z 522 (M+H)

Example 2052-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(methyl-phenyl-amino)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.55 (d, 1H, J=7.9 Hz), 7.53 (dd, 1H, J=8.2, 8.2 Hz) 7.29-7.23 (m, 3H),7.10-7.01 (m, 3H), 6.83 (m, 2H), 6.48 (bs, 1H), 5.42 (bt, 1H), 3.88 (d,2H, J=6.0 Hz), 3.38 (s, 3H), 3.37 (q, 1H, J=7.1 Hz), 3.04 (s, 3H), 1.43(d, 3H, J=7.1 Hz); IR (neat) 2923, 1654, 1590, 1509, 1462, 1398, 1338,1270, 1156, 973, 929, 758 cm⁻¹; MS (FAB) m/z 525 (M+H)

Example 2062-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6-trifluoromethyl-2-(4-trifluoromethyl-benzyloxy)-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.64 (d, 1H, J=8.4 Hz), 7.61 (d, 2H, J=8.6 Hz), 7.55 (d, 2H, J=8.1 Hz),7.49 (dd, 1H, J=8.2, 8.2 Hz), 7.25 (d, 1H, J=8.3 Hz), 7.07 (dd, 1H,J=11.2, 2.0 Hz), 7.01 (d, 1H, J=7.9 Hz), 6.43 (bs, 1H), 5.89 (bt, 1H),5.46 (m, 2H), 4.42 (d, 2H, J=6.0 Hz), 3.48 (q, 1H, J=7.1 Hz), 3.02 (s,3H), 1.45 (d, 3H, J=7.1 Hz); IR (neat) 3369, 1657, 1511, 1419, 1326,1267, 1159, 1119, 1067, 975, 934, 826 cm⁻¹, MS (FAB) m/z 594 (M+H)

Example 207N-{6-(chloro-difluoro-methyl)-2-[4-(1-vinyl-propenyl)-piperazin-1-yl]-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CD₃OD)

8.60 (m, 1H), 7.58 (d, 1H, J=7.5 Hz), 7.25-7.47 (m, 4H), 7.00-7.25 (m,4H), 4.35-4.57 (m, 2H), 3.73 (m, 1H, J=7.1 Hz), 3.32-3.45 (m, 8H), 2.95(s, 3H), 1.47 (d, 3H, J=7.1 Hz); IR (KBr) 2919, 1646, 1592, 1506, 1446,1332 cm⁻¹; MS (FAB) m/z 596 (M+H)

Example 208N-[6-(chloro-difluoro-methyl)-2-isobutoxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.48-7.58 (m, 2H), 7.16 (d, 1H, J=7.5 Hz),7.11 (m, 1H), 7.06 (m, 1H), 6.46 (m, 1H), 5.95 (bt, 1H), 4.32-4.44 (m,2H), 4.06-4.19 (m, 2H), 3.51 (q, 1H, J=7.1 Hz), 3.04 (s, 3H), 2.05 (m,1H), 1.49 (d, 3H, J=7.1 Hz), 0.99 (d, 6H, J=6.8 Hz); IR (KBr) 3291,2964, 1654, 1601, 1512, 1424, 1335, 1267, 1159, 1114, 1012, 971, 881,824 cm⁻¹; MS (FAB) m/z 508 (M+H)

Example 209N-(2-benzyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.44 (dd, 1H, J=8.4, 8.4 Hz), 7.41-7.34 (m,5H), 7.33 (d, 1H, J=8.6 Hz), 7.19 (d, 1H, J=7.9 Hz), 7.14 (s, 1H), 7.05(dd, 1H, J=11.3, 2.0 Hz), 6.95 (d, 1H, J=6.4 Hz), 6.41 (bs, 1H), 5.94(bt, 1H), 5.08 (s, 2H), 4.46 (m, 2H), 3.41 (q, 1H, J=7.0 Hz), 2.99 (s,3H), 1.43 (d, 3H, J=7.1 Hz); IR (neat) 3292, 1652, 1510, 1426, 1329,1240, 1159, 1122, 907, 742 cm⁻¹; MS (FAB) m/z 525 (M+H)

Example 210N-(4,4-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.53 (dd, 1H, J=8.4, 8.4 Hz), 7.48 (d, 1H, J=7.6 Hz), 7.21 (d, 1H, J=7.5Hz), 7.14 (dd, 1H, J=11.4, 1.9 Hz), 7.09 (d, 1H, J=8.8 Hz), 6.47 (bs,1H), 6.26 (bt, 1H), 4.47 (d, 2H, J=5.0 Hz), 3.56 (q, 1H, J=7.1 Hz),3.08-3.04 (m, 4H), 3.03 (s, 3H), 1.53 (d, 3H, J=7.1 Hz), 1.48-1.43 (m,4H), 0.99 (s, 6H); IR (neat) 3289, 2922, 1709, 1655, 1591, 1512, 1457,1420, 1336, 1159, 957, 834, 763 cm⁻¹; MS (FAB) m/z 531 (M+H)

Example 2112-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-3-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

8.69 (m, 2H), 7.79 (d, 1H, J=7.7 Hz), 7.64 (d, 1H, J=7.5 Hz), 7.48 (dd,1H, J=8.1 Hz), 7.34 (m, 1H), 7.25 (d, 1H, J=7.5 Hz), 7.05 (dd, 1H,J=11.4, 1.9 Hz), 7.02 (d, 1H, J=8.4 Hz), 5.87 (bt, 1H), 5.41 (s, 2H),4.38 (d, 2H, J=6.2 Hz), 3.49 (q, 1H, J=7.3 Hz), 3.04 (s, 3H), 1.46 (d,3H, J=7.1 Hz); IR (neat) 3299, 1658, 1601, 1511, 1416, 1335, 1267, 1156,974, 740 cm⁻¹; MS (FAB) m/z 527 (M+H)

Example 2122-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(3-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-pyridin-3-ylmethyl}-propionamide

¹H NMR (300 MHz, CDCl₃)

8.50 (d, 1H, J=3.6 Hz), 7.91 (dd, 1H, J=7.8, 1.8 Hz), 7.54 (d, 1H, J=6.9Hz), 7.49 (dd, 1H, J=8.1, 8.1 Hz), 7.05-7.17 (m, 4H), 6.40 (bt, 1H),4.52 (d, 2H, J=5.7 Hz), 3.61 (q, 1H, J=6.9 Hz), 3.35 (m, 8H), 3.02 (s,3H), 1.53 (d, 3H, J=6.9 Hz); IR (KBr) 3290, 2851, 1657, 1590,

Example 2162-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide)

¹H NMR (300 MHz, CDCl₃) δ 7.46 (dd, 1H, J=8.4, 8.4 Hz), 7.28-7.35 (m,5H), 7.13 (m, 1H), 7.07 (d, 1H, J=8.4 Hz), 6.89-6.99 (m, 3H), 6.32 (bt,1H), 4.53-4.67 (m, 2H), 3.55 (q, 1H, J=7.1 Hz), 3.20-3.28 (m, 4H),3.00-3.08 (m, 4H), 2.98 (s, 3H), 1.51 (d, 3H, J=6.9 Hz); IR (KBr) 2829,1652, 1598, 1506, 1425, 1335, 1230, 1159, 1122, 962, 911, 733 cm⁻¹; MS(FAB) m/z 579 (M+H)

Example 217N-(2-azocan-1-yl-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.52 (dd, 1H, J=8.3, 8.3 Hz), 7.38 (s, 1H),7.22-7.25 (m, 2H), 7.15 (dd, 1H, J=11.2, 2.0 Hz), 7.11 (d, 1H, J=8.1Hz), 6.51 (bs, 1H), 6.01 (bt, 1H), 4.55 (d, 2H, J=5.7 Hz), 3.55 (q, 1H,J=7.5 Hz), 3.00-3.05 (m, 7H), 1.62-1.72 (m, 10H), 1.53 (d, 3H, J=7.1Hz); IR (KBr) 3289, 2926, 1651, 1510, 1420, 1334, 1214, 1160, 1122, 975,908, 732 cm⁻¹; MS (FAB) m/z 530 (M+H)

Example 218N-[2-(4,4-dimethyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.51 (dd, 1H, J=8.3, 8.3 Hz), 7.32 (s, 1H), 7.21-7.30 (m, 2H), 7.14 (dd,1H, J=11.2, 1.8 Hz), 7.08 (d, 1H, J=8.6 Hz), 6.52 (bs, 2H), 4.45-4.60(m, 2H), 3.54 (q, 1H, J=7.1 Hz), 3.02 (s, 3H), 2.75-2.85 (m, 4H), 1.52(d, 3H, J=7.1 Hz), 1.42-1.50 (m, 4H), 1.00 (s, 6H); IR (KBr) 3284, 2922,1652, 1509, 1424, 1337, 1224, 1160, 1122, 1078, 973, 894, 827, 758 cm⁻¹;MS (FAB) m/z 530 (M+H)

Example 2192-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-p-tolyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.55 (m, 1H), 7.41 (d, 1H, J=7.8 Hz), 7.24-7.32 (m, 2H), 6.96-7.12 (m,4H), 6.78-6.81 (m, 3H), 4.40 (d, 2H, J=5.7 Hz), 3.56 (q, 1H, J=6.9 Hz),3.12 (m, 8H), 2.86 (s, 3H), 2.18 (s, 3H), 1.40 (d, 3H, J=6.9 Hz); IR(KBr) 3292, 2923, 1659, 1591, 1514, 1418, 1374, 1335, 1235, 1155, 968,817, 757 cm⁻¹; MS (FAB) m/z 594(M+H)

Example 2202-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-m-tolyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.45-7.54 (m, 2H), 7.06-7.28 (m, 4H), 6.73-6.76 (m, 3H), 6.28 (bs, 1H),6.20 (bt, 1H), 4.52 (d, 2H, J=5.7 Hz), 3.56 (q, 1H, J=6.9 Hz), 3.24 (m,8H), 2.98 (s, 3H), 2.35 (s, 3H), 1.52 (d, 3H, J=6.9 Hz);

IR (KBr) 3292, 2923, 1659, 1591, 1514, 1418, 1374, 1335, 1235, 1155,968, 817, 757 cm¹; MS (FAB) m/z 594 (M+H)

Example 2212-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide

¹H NMR (300 MHz, CDCl₃)

7.45-7.54 (m, 2H), 7.26 (d, 1H, J=7.5 Hz), 7.06-7.14 (m, 2H), 6.85-6.93(m, 4H), 6.41 (bs, 1H), 6.23 (bt, 1H), 4.53 (d, 2H, J=5.7 Hz), 3.79 (s,3H), 3.56 (q, 1H, J=6.9 Hz), 3.79 (m, 4H), 3.12 (m, 4H), 2.99 (s, 3H),1.51 (d, 3H, J=6.9 Hz); IR (KBr) 3294, 2839, 1659, 1591, 1511, 1418,1335, 1242, 1155, 1034, 968, 828, 757 cm⁻¹; MS (FAB) m/z 610 (M+H)

Example 2222-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-pyridin-3-ylmethyl}propionamide

¹H NMR (300 MHz, CD₃OD)

7.39-7.52 (m, 5H), 7.27 (d, 1H, J=7.8 Hz), 7.11-7.20 (m, 2H), 4.46 (d,2H, J=5.7 Hz), 3.67 (q, 1H, J=6.9 Hz), 3.33-3.38 (m, 8H), 3.00 (s, 3H),1.53 (d, 3H, J=6.9 Hz); IR (KBr) 3295, 2922, 1647, 1616, 1514, 1416,1331, 1234, 1156, 1115, 968, 829, 757 cm⁻¹; MS (FAB) m/z 648 (M+H)

Example 223N-(2-benzyloxy-6-tert-butyl-4-hydroxymethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.35-7.52 (m, 6H), 6.88-6.99 (m, 3H), 6.54 (bs1H), 6.32 (bt, 1H), 5.46 (d, 1H, J=16.3 Hz), 5.34 (d, 1H, J=16.3 Hz),4.65 (m, 2H), 4.35 (d, 2H, J=5.7 Hz), 3.32 (q, 1H, J=6.9 Hz), 2.98 (s,3H), 1.35 (d, 3H, J=6.9 Hz), 1.30 (s, 9H); IR (KBr) 3368, 2960, 1648,1592, 1512, 1449, 1398, 1333, 1157, 1027, 973, 756 cm⁻¹; MS (FAB) m/z544 (M+H)

Example 2252-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.57 (d, 1H, J=7.5 Hz), 7.52 (dd, 1H, J=8.2, 8.2 Hz),7.19 (d, 1H, J=7.4 Hz), 7.12-7.05 (m, 2H), 6.45 (bs, NH), 5.98 (bt, NH),4.38-4.29 (m, 4H), 3.51 (q, 1H, J=7.0 Hz), 3.03 (s, 3H), 1.77-1.67 (m,2H), 1.49 (d, 3H, J=7.1 Hz), 1.43-1.35 (m, 4H), 0.93 (t, 3H, J=7.1 Hz);IR(neat) 3287, 2959, 1656, 1604, 1513, 1464, 1425, 1337, 1269, 1157, 977cm⁻¹; Mass (FAB) m/z 506[M+H]

Example 226 2,2-dimethyl-propionic acid3′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-ylester

¹H NMR (CDCl₃) δ 7.54-7.47 (m, 2H), 7.22 (d, 1H, J=7.7 Hz), 7.15 (dd,1H, J 11.0, 1.8 Hz), 7.10 (m, 1H), 6.49 (bs, NH), 6.01 (bt, NH), 4.94(m, 1H), 4.47 (d, 2H, J=6.0 Hz), 3.58 (q, 1H, J=7.0 Hz), 3.32-3.22 (m,2H), 3.13-3.03 (m, 2H), 3.04 (s, 3H), 2.00-1.90 (m, 2H), 1.82-1.70 (m,2H), 1.55 (d, 3H, J=7.1 Hz), 1.21 (s, 9H); IR (neat) 3300, 2973, 1715,1656, 1513, 1420, 1336, 1284, 1163, 759 cm⁻¹; MS (FAB) m/z 603 (M+H)

Example 2272-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-oxo-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide3′-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.55-7.49 (m, 2H), 7.29 (d, 1H, J=7.9 Hz), 7.17 (dd,1H, J=11.2, 2.0 Hz), 7.11 (d, 1H, J=8.6 Hz), 6.70 (bs, NH), 6.04 (bt,NH), 4.54 (d, 2H, J=5.7 Hz), 3.61 (q, 1H, J=7.0 Hz), 3.49 (t, 4H, J=6.0Hz), 3.04 (s, 3H), 2.55 (t, 4H, J=6.1 Hz), 1.55 (d, 3H, J=7.1 Hz); IR(neat) 3294, 1712, 1658, 1592, 1513, 1418, 1335, 1156, 733 cm⁻¹; MS(FAB) m/z 517 (M+H)

Example 228N-(4-ethoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.55-7.48 (m, 2H), 7.23 (d, 1H, J=7.7 Hz), 7.15-7.08(m, 2H), 6.54 (bs, NH), 6.23 (bt, NH), 4.48 (d, 2H), 3.58-3.23 (m, 6H),3.04 (s, 3H), 2.94-2.86 (m, 2H), 2.05-1.95 (m, 2H), 1.63-1.50 (m, 2H),1.53 (d, 3H, J=7.1 Hz), 1.24 (t, 3H, J=7.0 Hz); IR (neat) 3290, 2929,1655, 1513, 1419, 1335, 1158 cm⁻¹; MS (FAB) m/z 547 (M+H)

Example 229N-[2-(4-ethyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.51 (dd, 1H, J=8.3, 8.3 Hz), 7.29 (s, 1H), 7.21-7.27 (m, 2H), 7.14 (m,1H), 7.08 (d, 1H, J=8.4 Hz), 6.48-6.59 (m, 2H), 4.46-4.60 (m, 2H), 3.53(q, 1H, J=6.9 Hz), 2.91-3.07 (m, 5H), 2.58-2.61 (m, 2H), 1.75-1.86 (m,2H), 1.52 (d, 3H, J=7.1 Hz), 1.10-1.37 (m, 5H), 0.93 (t, 3H, J=7.0 Hz);IR (KBr) 3285, 2930, 1652, 1509, 1423, 1336, 1160, 1122, 973, 910, 733cm⁻¹; MS (FAB) m/z 530 (M+H)

Example 2302-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-trifluoromethyl-2-(4-trifluoromethyl-piperidin-1-yl)-benzyl]-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.52 (dd, 1H, J=8.2, 8.2 Hz), 7.22-7.32 (m,3H), 7.12-7.19 (m, 1H), 7.09 (d, 1H, J=8.3 Hz), 6.52 (bs, 1H), 6.12 (bt,1H), 4.52 (d, 2H, J=5.9 Hz), 3.56 (q, 1H, J=7.1 Hz), 3.05-3.15 (m, 2H),3.03 (bs, 3H), 2.62-2.77 (m, 2H), 2.08-2.24 (m, 1H), 1.93-2.02 (m, 2H),1.61-1.74 (m, 2H), 1.54 (d, 3H, J=7.1 Hz); IR (KBr) 3289, 2936, 1653,1510, 1425, 1334, 1254, 1158, 1081, 972, 907, 825, 733 cm⁻¹; MS (FAB)m/z 570 (M+H)

Example 231N-[2-(4-benzyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.52 (dd, 1H, J=8.2, 8.2 Hz), 7.27-7.35 (m, 3H), 7.20-7.26 (m, 2H),7.11-7.19 (m, 4H), 7.08 (d, 1H, J=8.2 Hz), 6.38-6.46 (m, 2H), 4.51 (d,2H, J=5.7 Hz), 3.52 (q, 1H, J=7.1 Hz), 2.85-3.05 (m, 5H), 2.55-2.70 (m,4H), 1.60-1.80 (m, 3H), 1.52 (d, 3H, J=7.1 Hz), 1.21-1.38 (m, 2H); IR(KBr) 3292, 2923, 1652, 1509, 1424, 1336, 1160, 1121, 973, 909, 734, 701cm⁻¹; MS (FAB) m/z 592 (M+H)

Example 233N-(6-tert-butyl-2-cyclohexyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.50 (dd, 1H, J=8.3, 8.3 Hz), 7.36 (d, 1H, J=7.3 Hz),7.14-7.05 (m, 2H), 6.77 (d, 1H, J=7.5 Hz), 6.70 (bs, NH), 6.14 (bt, NH),5.10 (m, 1H), 4.39-4.23 (m, 2H), 3.49 (q, 1H, J=7.1 Hz), 3.02 (s, 3H),1.92 (m, 2H), 1.71 (m, 2H), 1.60-1.25 (m, 6H), 1.48 (d, 1H, J=7.1 Hz),1.28 (s, 9H); IR (neat) 3288, 2935, 2859, 1652, 1585, 1513, 1451, 1406,1335, 1254, 1159, 733 cm⁻¹; MS (FAB) m/z 506 (M+H)

Example 234N-(6-tert-butyl-2-cyclopentyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.50 (dd, 1H, J=8.3, 8.3 Hz), 7.35 (d, 1H, J=7.7 Hz),7.14-7.05 (m, 2H), 6.77 (d, 1H, J=7.5 Hz), 6.59 (bs, NH), 6.03 (bt, NH),5.44 (m, 1H), 4.36-4.21 (m, 1H), 3.48 (q, 1H, J=6.8 Hz), 3.02 (s, 3H),1.96 (m, 2H), 1.75-1.60 (m, 6H), 1.48 (d, 3H, J=7.1 Hz), 1.29 (s, 9H);IR (neat) 3291, 2962, 1652, 1513, 1452, 1406, 1337, 1255, 1159, 982cm⁻¹; MS (FAB) m/z 492 (M+H)

Example 235N-(2-butoxy-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.50 (dd, 1H, J=8.4, 8.4 Hz), 7.36 (d, 1H, J=7.5 Hz),7.15-7.05 (m, 2H), 6.79 (d, 1H, J=7.5 Hz), 6.59 (bs, NH), 6.06 (bt, NH),4.39-4.23 (m, 4H), 3.48 (q, 1H, J=7.3 Hz), 3.02 (s, 3H), 1.69 (m, 2H),1.48 (d, 3H, J=7.1 Hz), 1.43 (m, 2H), 1.29 (s, 9H), 0.97 (t, 3H, J=7.3Hz); IR (neat) 3289, 2959, 1651, 1585, 1513, 1455, 1410, 1337, 1254,1159 cm⁻¹; MS (FAB) m/z 480 (M+H)

Example 236N-(6-tert-butyl-2-hexyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.50 (dd, 1H, J=8.4, 8.4 Hz), 7.36 (d, 1H, J=7.5 Hz),7.15-7.05 (m, 2H), 6.79 (d, 1H, J=7.5 Hz), 6.58 (bs, NH), 6.07 (bt, NH),4.39-4.24 (m, 4H), 3.48 (q, 1H, J=7.0 Hz), 3.02 (s, 3H), 1.71 (m, 2H),1.48 (d, 3H, J=7.1 Hz), 1.45-1.25 (m, 6H), 1.29 (s, 9H), 0.91 (m, 3H);IR (neat) 3289, 2957, 1651, 1585, 1513, 1455, 1411, 1338, 1254, 1159,973 cm⁻¹; MS (FAB) m/z 508 (M+H)

Example 237N-(2-benzyloxy-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.46-7.30 (m, 7H), 7.06 (dd, 1H, J=11.2, 1.8 Hz), 6.95(d, 1H, J=8.4 Hz), 6.84 (d, 1H, J=7.5 Hz), 6.53 (bs, NH), 6.06 (bt, NH),5.42 (m, 2H), 4.42-4.26 (m, 2H), 3.38 (q, 1H, J=7.1 Hz), 2.98 (s, 3H),1.41 (d, 3H, J=7.1 Hz), 1.30 (s, 9H); IR (neat) 3291, 2959, 1652, 1512,1452, 1405, 1338, 1254, 1158 cm⁻¹; MS (FAB) m/z 514 (M+H)

Example 238N-(2-cyclohexyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.51 (dd, 1H, J=8.4, 8.4 Hz), 7.30 (m, 1H), 7.09-7.10 (m, 2H), 7.06 (d,1H, J=8.3 Hz), 7.02 (bs, 1H), 6.47 (bs, 1H), 5.53 (m, 1H), 4.27-4.50 (m,3H), 3.50 (q, 1H, J=7.0 Hz), 3.02 (s, 3H), 1.84-1.96 (m, 2H), 1.64-1.78(m, 2H), 1.25-1.63 (m, 9H); IR (KBr) 3289, 2937, 2859, 1653, 1510, 1427,1330, 1236, 1160, 1124, 1043, 973, 906, 733 cm⁻¹; MS (FAB) m/z 517 (M+H)

Example 240N-(6-tert-butyl-2-pyrrolidin-1-yl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methansulfonylamino-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.51 (dd, 1H, J=8.3, 8.3 Hz), 7.24 (d, 1H, J=7.7 Hz), 7.20 (dd, 1H,J=11.0, 2.0 Hz), 7.08 (d, 1H, J=8.8 Hz), 6.67 (d, 1H, J=7.7 Hz), 6.50(bs, 1H), 5.90 (bs, 1H), 4.4 (d, 2H, J=4.6 Hz), 3.5 (q, 1H, J=7.0 Hz),3.41-3.36 (m, 4H), 3.00 (s, 3H), 1.85-1.80 (m, 4H), 1.50 (d, 3H, J=7.1Hz), 1.30 (s, 9H); IR (KBr) 3289, 2962, 2868, 1650, 1513, 1450, 1411cm⁻¹; MS (FAB) m/z 477 (M+H)

Example 241N-(6′-tert-butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.51 (dd, 1H, J=8.3, 8.3 Hz), 7.30 (d, 1H, J=7.7 Hz), 7.20-7.00 (m, 2H),6.90 (d, 1H, J=7.7 Hz), 4.45 (m, 2H), 3.52 (q, 1H, J=7.0 Hz), 3.30 (m,2H), 3.00 (s, 3H), 2.78 (m, 2H), 1.70-1.50 (m, 5H), 1.50 (d, 3H, J=7.1Hz), 1.30 (s, 9H), 0.97 (d, 3H, J=6.6 Hz); IR (KBr) 3291, 2922, 1651,1513, 1452, 1400, 1335 cm⁻¹; MS (FAB) m/z 505 (M+H)

Example 243N-[2-(4-butyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.61 (d, 1H, J=7.5 Hz), 7.48 (dd, 1H, J=8.2, 8.2 Hz), 7.33 (d, 2H, J=8.1Hz), 7.23 (d, 1H, J=7.3 Hz), 7.10 (d, 2H, J=7.9 Hz), 7.04 (dd, 1H,J=11.2, 2.0 Hz), 6.97 (d, 1H, J=8.6 Hz), 6.41 (bs, 1H), 5.94 (bt, 1H),5.38 (m, 2H), 4.37 (m, 2H), 3.39 (q, 1H, J=7.0 Hz), 3.01 (s, 3H), 2.63(t, 2H, J=7.8 Hz), 1.61 (m, 2H), 1.41 (d, 3H, J=7.1 Hz), 1.38 (m, 2H),0.93 (t, 3H, J=7.3 Hz); IR (neat) 3289, 2930, 1655, 1602, 1512, 1463,1420, 1352, 1267, 1158, 975, 933, 831, 761 cm⁻¹; MS (FAB) m/z 582 (M+H)

Example 244N-[2-(4-tert-butyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.61 (d, 1H, J=7.1 Hz), 7.48 (dd, 1H, J=8.3,8.3 Hz), 7.45-7.37 (m, 4H), 7.23 (d, 1H, J=7.3 Hz), 7.04 (dd, 1H,J=11.2, 1.9 Hz), 6.97 (d, 1H, J=8.1 Hz), 6.42 (bs, 1H), 5.98 (bt, 1H),5.39 (m, 2H), 4.38 (m, 2H), 3.40 (q, 1H, J=7.3 Hz), 3.00 (s, 3H), 1.41(d, 3H, J=7.1 Hz), 1.34 (s, 9H); IR (neat) 3293, 2964, 1656, 1601, 1513,1462, 1422, 1348, 1267, 1156, 976, 833, 758 cm⁻¹; MS (FAB) m/z 582 (M+H)

Example 2452-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(indan-2-yloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.59 (d, 1H, J=7.3 Hz), 7.46 (dd, 1H, J=8.2, 8.2 Hz), 7.29-7.24 (m, 5H),6.99 (dd, 1H, J=11.2, 2.0 Hz), 6.91 (d, 1H, J=8.8 Hz), 6.35 (bs, 1H),5.89 (m, 1H), 5.79 (bt, 1H), 4.27 (m, 2H), 3.43 (dd, 2H, J=17.2, 5.5Hz), 3.08-3.04 (m, 3H), 3.00 (s, 3H), 1.31 (d, 3H, J=7.1 Hz)

IR (neat) 3291, 2927, 1658, 1600, 1511, 1418, 1339, 1268, 1157, 1015,970, 933, 747 cm⁻¹; MS (FAB) m/z 552 (M+H)

Example 2462-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-p-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.46 (dd, 1H, J=8.2, 8.2 Hz), 7.34 (s, 1H), 7.33 (d, 1H, J=7.5 Hz), 7.31(d, 1H, J=7.0 Hz), 7.13 (d, 2H, J=8.1 Hz), 7.14 (dd, 1H, J=11.2, 2.0Hz), 7.08 (d, 1H, J=10.0 Hz), 6.86 (d, 2H, J=8.6 Hz), 6.35 (bt, 2H),6.22 (bs, 1H), 4.57 (m, 2H), 3.54 (q, 1H, J=7.0 Hz), 3.18-3.12 (m, 4H),3.05-3.01 (m, 4H), 2.97 (s, 3H), 2.31 (s, 3H), 1.51 (d, 3H, J=7.1 Hz);IR (neat) 2923, 1655, 1513, 1425, 1334, 1221, 1159, 1123, 963, 816, 757cm⁻¹; MS (FAB) m/z 593 (M+H)

Example 2472-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-m-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.46 (dd, 1H, J=8.2 Hz), 7.36-7.26 (m, 3H),7.21 (m, 1H), 7.13 (dd, 1H, J=11.2, 2.0 Hz), 7.07 (d, 1H, J=8.1, 8.1Hz), 6.79-6.74 (m, 3H), 6.33 (bt, 2H), 6.25 (bs, 1H), 4.57 (m, 2H), 3.54(q, 1H, J=7.1 Hz), 3.24-3.18 (m, 4H), 3.08-3.01 (m, 4H), 2.97 (s, 3H),2.36 (s, 3H), 1.51 (d, 3H, J=7.1 Hz); IR (neat) 3294, 2921, 1653, 1603,1509, 1425, 1335, 1249, 1159, 1122, 965, 775 cm⁻¹; MS (FAB) m/z 593(M+H)

Example 2482-(3-fluoro-4-methylsulfonamido-phenyl)-N-{4-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-benzyl}-propionamide

¹H NMR (300 MHz, CDCl₃)

7.53 (d, 2H, J=8.6 Hz), 7.50 (dd, 1H, J=8.3, 8.3 Hz), 7.33 (s, 1H), 7.30(d, 2H, J=8.2 Hz), 7.14 (dd, 1H, J=11.2, 2.0 Hz), 7.08 (d, 1H, J=10.0Hz), 6.97 (d, 2H, J=8.9 Hz), 6.23 (bt, 1H), 4.58 (d, 2H, J=6.4 Hz), 3.54(q, 1H, J=7.1 Hz), 3.39-3.31 (m, 4H), 3.04-2.98 (m, 4H), 3.01 (s, 3H),1.53 (d, 3H, J=7.1 Hz); IR (neat) 2923, 1652, 1615, 1511, 1423, 1331,1237, 1159, 1117, 961, 827 cm⁻¹; MS (FAB) m/z 647 (M+H)

Example 2492-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-4-trifluoromethyl-benzyl}-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47 (dd, 1H, J=8.2, 8.2 Hz), 7.33 (d, 2H, J=10.1 Hz), 7.29 (s, 1H),7.13 (dd, 1H, J=11.2, 2.0 Hz), 7.07 (d, 1H, J=8.3 Hz), 6.98-6.85 (m,4H), 6.35 (bs, 1H), 6.33 (bt, 1H), 4.59 (m, 2H), 3.80 (s, 3H), 3.54 (q,1H, J=7.1 Hz), 3.15-3.08 (m, 4H), 3.05-2.98 (m, 4H), 2.98 (s, 3H), 1.51(d, 3H, J=7.1 Hz); IR (neat) 2929, 1657, 1511, 1425, 1335, 1244, 1159,1122, 1036, 963, 827, 757 cm⁻¹; MS (FAB) m/z 609 (M+H)

Example 2552-(3-fluoro-4-methylsulfonamiclo-phenyl)-N-{2-[4-(4-fluoro-phenyl)-piperidin-1-yl]-4-trifluoromethyl-benzyl}-propionamide

¹H NMR (300 MHz, CDCl₃)

7.50 (dd, 1H, J=8.3 Hz), 7.30-7.26 (m, 3H), 7.23-7.18 (m, 2H), 7.15 (dd,1H, J=11.8, 2.0 Hz), 7.08 (d, 1H, J=10.0 Hz), 7.03 (m, 2H), 6.46 (bs,1H), 6.24 (bt, 1H), 4.56 (d, 2H, J=5.7 Hz), 3.56 (q, 1H, J=7.1 Hz), 3.09(m, 2H), 3.00 (s, 3H), 2.83 (m, 2H), 2.64 (m, 1H), 1.94 (m, 2H), 1.78(m, 2H), 1.54 (d, 3H, J=6.9 Hz); IR (neat) 3320, 2922, 1652, 1509, 1423,1332, 1222, 1159, 1120, 971, 888, 834, 763 cm⁻¹; MS (FAB) m/z 596 (M+H)

Example 256N-(2-butoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.55 (d, 1H, J=7.5 Hz), 7.40 (d, 1H, J=8.8 Hz), 7.17 (d, 1H, J=7.3 Hz),7.11 (d, 1H, J=6.9 Hz), 7.10 (s, 1H), 6.21 (bs, 1H), 5.93 (bt, 1H), 4.36(d, 2H, J=6.4 Hz), 4.31 (m, 2H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s, 3H),2.28 (s, 3H), 1.69 (m, 2H), 1.48 (d, 3H, J=7.1 Hz), 1.41 (m, 2H), 0.96(t, 3H, J=7.3 Hz); IR (neat) 3291, 2963, 1654, 1605, 1537, 1463, 1425,1326, 1151, 972, 932, 834 cm⁻¹; MS (FAB) m/z 488 (M+H)

Example 257N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.54 (d, 1H, J=7.5 Hz), 7.39 (d, 1H, J=9.0 Hz), 7.17 (d, 1H, J=7.3 Hz),7.11 (d, 1H, J=7.0 Hz), 7.09 (s, 1H), 6.21 (bs, 1H), 5.94 (bt, 1H), 4.36(d, 2H, J=6.2 Hz), 4.30 (m, 2H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s, 3H),2.28 (s, 3H), 1.69 (m, 2H), 1.48 (d, 3H, J=7.1 Hz), 1.39-1.26 (m, 6H),0.91 (t, 3H, J=6.6 Hz); IR (neat) 3290, 2931, 1655, 1604, 1504, 1464

Example 258N-[2-(4-chloro-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.60 (d, 1H, J=7.5 Hz), 7.48 (dd, 1H, J=8.3, 8.3 Hz), 7.39-7.28 (m, 4H),7.24 (d, 1H, J=7.5 Hz), 7.05 (dd, 1H, J=11.2, 2.0 Hz), 7.00 (d, 1H,J=8.3 Hz), 6.48 (bs, 1H), 5.91 (bt, 1H), 5.37 (d, 2H, J=4.7 Hz), 4.39(m, 2H), 3.45 (q, 1H, J=7.1 Hz), 3.02 (s, 3H), 1.44 (d, 3H, J=7.0 Hz);IR (neat) 3299, 2929, 1658, 1601, 1512, 1461, 1423, 1350, 1267, 7756,975, 934, 808 cm⁻¹; MS (FAB) m/z 560 (M+H)

Example 259N-(4-dimethylaminomethyl-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7A5-7.50 (m, 2H), 7.36 (m, 4H), 7.21 (m, 1H), 7.18 (d, 1H, J=8.1 Hz),7.13 (dd, 1H, J=11.1, 1.8 Hz), 7.06 (d, 1H, J=8.1 Hz), 6.37 (bt, 1H),4.46 (d, 2H, J=5.7 Hz), 3.58 (q, 1H, J=6.9 Hz), 3.17 (m, 2H), 3.01 (s,3H), 2.98 (m, 2H), 2.52 (s, 2H), 2.18 (m, 2H), 1.98 (s, 6H), 1.51 (d,3H, J=6.9 Hz); IR (KBr) 2937, 1657, 1592, 1509, 1456, 1420, 1335, 1252,1157, 1041, 972, 758, 702 cm⁻¹; MS (FAB) m/z 636 (M+H)

Example 260N-[2-(4-cyclohexyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47-7.53 (m, 2H), 7.23 (d, 1H, J=7.8 Hz), 7.07-7.15 (m, 2H), 6.26 (bt,1H), 4.44 (d, 2H, J=5.7 Hz), 3.58 (q, 1H, J=6.9 Hz), 3.27 (m, 4H), 3.03(s, 3H), 2.84 (m, 4H), 2.50 (m, 1H), 1.94 (m, 2H), 1.85 (m, 2H), 1.51(d, 3H, J=6.9 Hz), 1.25-1.30 (m, 6H); IR (KBr)) 2934, 2857, 1657, 1591,1502, 1459, 1418, 1334, 1271, 1152, 979, 757 cm⁻¹; MS (FAB) m/z 586(M+H)

Example 261N-(6-tert-butyl-2-cyclopentyloxy-4-hydroxymethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48 (dd, 1H, J=8.1, 8.1 Hz), 6.99-7.05 (m, 2H), 6.82 (s, 1H), 6.32 (bt,1H), 5.40 (m, 1H), 4.63 (d, 2H, J=5.7 Hz), 4.37 (m, 2H), 3.47 (q, 1H,J=6.9 Hz), 3.03 (s, 3H), 1.94 (m, 2H), 1.63 (m, 6H), 1.45 (d, 3H, J=6.9Hz), 1.29 (s, 9H); IR (KBr) 3369, 2962, 1651, 1592, 1513, 1452, 1397,1336, 1158, 1026, 974, 758 cm⁻¹; MS (FAB) m/z 522 (M+H)

Example 2622-(4-methylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.46 (d, 1H, J=7.5 Hz), 7.23-7.31 (m, 2H), 7.14-7.22 (m, 3H), 6.60 (bs,1H), 6.20 (bt, 1H), 4.46 (d, 2H, J=5.9 Hz), 3.59 (q, 1H, J=7.1 Hz),3.19-3.38 (m, 2H), 3.01 (s, 3H), 2.75-2.87 (m, 2H), 1.65-1.79 (m, 2H),1.48-1.56 (m, 4H), 1.14-1.32 (m, 2H), 0.97 (d, 3H, J=6.6 Hz); IR (KBr)3287, 2921, 1646, 1512, 1458, 1423, 1335, 1233, 1145, 970, 840 cm⁻¹; MS(FAB) m/z 499 (M+H)

Example 263N-[2-(3,3-dimethyl-butyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.49-7.58 (m, 2H), 7.43 (d, 1H, J=7.9 Hz), 7.17 (dd, 1H, J=11.2, 1.8Hz), 7.11 (d, 1H, J=8.6 Hz), 6.48 (bs, 1H), 5.70 (bt, 1H), 4.41-4.56 (m,2H), 3.58 (q, 1H, J=7.3 Hz), 3.04 (s, 3H), 2.71-2.79 (m, 2H), 1.51-1.60(m, 5H), 0.96 (s, 9H); IR (KBr) 3292, 2957, 1656, 1512, 1463, 1408,1340, 1277, 1157, 972, 906, 758 cm⁻¹; MS (FAB) m/z 504 (M+H)

Example 2642-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-p-tolyl-ethyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48-7.59 (m, 2H), 7.46 (m, 1H), 7.12 (dd, 1H, J=11.2, 2.0 Hz),6.96-7.10 (m, 5H), 6.41 (bs, 1H), 5.26 (bt, 1H), 4.20-4.39 (m, 2H), 3.35(q, 1H, J=7.1 Hz), 3.05-3.15 (m, 4H), 3.05 (s, 3H), 2.31 (s, 3H), 1.47(d, 3H, J=7.1 Hz); IR (KBr) 3298, 2925, 1658, 1589, 1513, 1408, 1339,1279, 1157, 973, 912, 813, 733 cm⁻¹; MS (FAB) m/z 538 (M+H)

Example 2672-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.50-7.59 (m, 2H), 7.44 (d, 1H, J=8.1 Hz), 7.16 (dd, 1H, J=11.2, 2.0Hz), 7.10 (d, 1H, J=8.4 Hz), 6.43 (bs, 1H), 5.70 (bt, 1H), 4.41-4.58 (m,2H), 3.57 (q, 1H, J=7.1 Hz), 3.04 (bs, 3H), 2.78 (t, 2H, J=7.9 Hz),1.61-1.74 (m, 2H), 1.53 (d, 3H, J=7.1 Hz), 1.21-1.43 (m, 6H), 0.88 (m,3H); IR (KBr) 3289, 2929, 2857, 1658, 1589, 1512, 1462, 1408, 1341,1277, 1158, 973, 908 cm⁻¹; MS (FAB) m/z 504 (M+H)

Example 2682-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-pentyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.51-7.58 (m, 2H), 7.44 (d, 1H, J=8.0 Hz),7.17 (dd, 1H, J=11.2, 2.0 Hz), 7.10 (d, 1H, J=8.4 Hz), 6.48 (bs, 1H),5.70 (bt, 1H), 4.41-4.57 (m, 2H), 3.57 (q, 1H, J=7.0 Hz), 3.04 (s, 3H),2.76 (t, 2H, J=8.0 Hz), 1.61-1.76 (m, 2H), 1.58 (m, 1H), 1.54 (d, 3H,J=7.1 Hz), 1.19-1.27 (m, 2H), 0.87 (d, 6H, J=6.6 Hz); IR (KBr) 3290,2956, 1656, 1589, 1512, 1462, 1408, 1339, 1279, 1158, 972, 906 cm⁻¹; MS(FAB) m/z 504 (M+H)

Example 2692-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-hydroxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.54-7.49 (m, 2H), 7.23 (d, 1H, J=7.7 Hz), 7.16-7.09(m, 2H), 6.69 (bs, NH), 6.25 (bt, NH), 4.48 (m, 2H), 3.84 (m, 1H), 3.58(q, 1H, J=7.3 Hz), 3.38-3.26 (m, 2H), 3.04 (s, 3H), 2.97-2.88 (m, 2H),2.02-1.92 (m, 2H), 1.75 (s, OH), 1.53 (d, 3H, J=7.1 Hz); IR (neat) 3294,2934, 1658, 1592, 1512, 1418, 1334, 1155, 732 cm⁻¹; Mass (FAB) m/z519[M+H]

Example 270N-(2-cyclohexylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.56 (d, 1H, J=7.3 Hz), 7.51 (dd, 1H, J=8.3, 8.3 Hz),7.18 (d, 1H, J=7.3 Hz), 7.12-7.04 (m, 2H), 6.57 (bs, NH), 5.99 (bt, NH),4.38 (m, H), 4.16 (m, 2H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s, 3H),1.82-1.67 (m, 5H), 1.49 (d, 3H, J=7.1 Hz), 1.32-1.00 (m, 6H); IR (neat)3292, 2928, 2854, 1656, 1513, 1425, 1338, 1269, 1158 cm⁻¹; MS (FAB) m/z532 (M+H)

Example 2712-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-cyclohexylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (CDCl₃) δ 7.56 (d, 1H, J=7.3 Hz), 7.50 (dd, 1H, J=8.2, 8.2 Hz),7.18 (d, 1H, J=7.5 Hz), 7.12-7.04 (m, 2H), 6.59 (bs, NH), 6.00 (bt, NH),4.45-4.11 (m, 4H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s, 3H), 1.95-1.25 (m,12H), 1.10-0.90 (m, 4H); IR (neat) 3295, 2924, 1655, 1513, 1425, 1337,1268, 1158 cm⁻¹; MS (FAB) m/z 546 (M+H)

Example 279N-[2-(2,2-dimethyl-cyclopropylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.58 (d, 1H, J=7.3 Hz), 7.51 (dd, 1H, J=8.4, 8.4 Hz),7.19 (d, 1H, J=7.3 Hz), 7.14-7.05 (m, 2H), 6.54 (bs, NH), 6.07 (bt, NH),4.57-4.33 (m, 3H), 4.24-4.15 (m, 1H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s,3H), 1.49 (dd, 3H, J=7.0, 1.7 Hz), 1.13 (d, 3H, J=1.5 Hz), 1.09 (s, 3H),1.06-0.95 (m, 1H), 0.57 (dd, 1H, J=8.4, 4.4 Hz), 0.28 (m, 1H); IR (neat)3293, 2928, 1655, 1514, 1427, 1339, 1266, 1158, 980 cm⁻¹; MS (FAB) m/z518(M+H)

Example 2822-(3-fluoro-4-methylsulfonamido-phenyl)-N-(3-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.54-7.47 (m, 2H), 7.21 (d, 1H, J=7.7 Hz), 7.15-7.07(m, 2H), 6.64 (bs, NH), 6.34 (bt, NH), 4.48 (d, 2H, J=5.9 Hz), 3.56 (q,1H, J=7.0 Hz), 3.32-3.17 (m, 2H), 3.03 (s, 3H), 2.74 (m, 1H), 2.46 (m,1H), 1.82-1.61 (m, 4H), 1.53 (d, 3H, J=7.1 Hz), 1.13-1.01 (m, 1H), 0.91(m, 3H); IR (neat) 3295, 2927, 1655, 1593, 1513, 1458, 1419, 1336, 1158cm⁻¹; MS (FAB) m/z 517 (M+H)

Example 2832-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.62-7.48 (m, 2H), 7.30 (m, 1H), 7.18-7.07 (m, 2H),6.71 (bt, NH), 6.58 (bs, NH), 4.67-4.57 (m, 1H), 4.35 (m, 1H), 3.56-3.46(m, 2H), 3.03 & 3.02 (s, 3H), 3.01-2.95 (m, 1H), 2.79 (m, 1H), 1.80-1.50(m, 9H), 0.90 & 0.85 (d, 3H); IR (neat) 3289, 2933, 2853, 1655, 1512,1456, 1411, 1335, 1158 cm⁻¹; MS (FAB) m/z 517 (M+H)

Example 2842-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-ethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.44-7.50 (m, 2H), 7.19 (d, 1H, J=7.8 Hz), 6.96-7.06 (m, 2H), 5.79 (bt,1H), 3.54 (q, 2H, J=6.3 Hz), 3.25-3.40 (m, 3H), 3.03 (s, 3H), 2.78-2.87(m, 4H), 1.76 (m, 2H), 1.60 (m, 3H), 1.42 (d, 3H, J=6.9 Hz), 0.99 (d,3H, J=6.6 Hz); IR (KBr) 2920, 1646, 1537, 1455, 1415, 1325, 1153, 832cm⁻¹; MS (FAB) m/z 531 (M+H)

Example 285N-(4-cyano-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.28-7.52 (m, 8H), 7.08-7.17 (m, 2H), 6.04 (bt, 1H), 4.49 (d, 2H, J=5.7Hz), 3.58 (q, 1H, J=6.9 Hz), 3.36-3.60 (m, 5H), 3.02 (s, 3H), 2.17 (m,4H), 1.54 (d, 3H, J=6.9 Hz); IR (KBr) 2931, 1657, 1590, 1509, 1455,1324, 1241, 1154, 966, 758, 702 cm⁻¹; MS (FAB) m/z 604(M+H)

Example 2872-(4-ethanesulfonylamino-3-fluoro-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.53 (dd, 1H, J=8.1, 8.1 Hz), 7.47 (d, 1H, J=7.5 Hz), 7.19 (d, 1H, J=7.5Hz), 7.11 (d, 1H, J=11.4, 1.8 Hz), 7.06 (d, 1H, 8.4 Hz), 6.55 (bs, 1H),6.30 (bt, 1H), 4.46 (d, 2H, J=5.7 Hz), 3.55 (q, 1H, J=6.9 Hz), 3.29 (m,2H), 3.11 (q, 2H, J=7.5 Hz), 2.80 (m, 2H), 1.67-1.70 (m, 3H), 1.52 (d,3H, J=6.9 Hz), 1.38 (t, 3H, J=7.5 Hz), 1.22 (m, 2H), 0.97 (d, 3H, J=6.3Hz); IR (KBr) 3290, 2926, 2658, 1592, 1511, 1456, 1418, 1374, 1335,1275, 1148, 942, 832, 757 cm⁻¹; MS (FAB) m/z 531(M+H)

Example 2882-(4-dimethylaminsulfonylamino-3-fluoro-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.45-7.52 (m, 2H), 7.18 (d, 1H, J=7.5 Hz), 7.02-7.10 (m, 2H), 6.26 (bs,1H), 4.46 (d, 2H, J=5.7 Hz), 4.55 (q, 1H, J=6.9 Hz), 3.30 (m, 2H),2.77-2.83 (m, 9H), 1.72 (m, 2H), 1.52 (d, 3H, J=6.9 Hz), 1.19-1.26 (m,3H), 0.97 (d, 3H, J=6.0 Hz); IR (KBr) 3293, 2923, 1658, 1592, 1512,1456, 1420, 1339, 1272, 1152, 959, 758 cm⁻¹; MS (FAB) m/z 546(M+H)

Example 2892-(4-methylsulfonamido-3-methoxy-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.48-7.45 (m, 2H), 7.18 (d, 1H, J=7.7 Hz), 6.89-6.83(m, 2H), 6.75 (bs, NH), 6.25 (bt, NH), 4.46 (d, 2H, J=5.7 Hz), 3.83 (s,3H), 3.57 (q, 1H, J=7.0 Hz), 3.33-3.21 (m, 2H), 2.95 (s, 3H), 2.84-2.76(m, 2H), 1.75-1.63 (m, 3H), 1.54 (d, 3H, J=7.1 Hz), 1.30-1.13 (m, 2H),0.97 (d, 3H, J=6.4 Hz); IR (neat) 3297, 2925, 1656, 1594, 1512, 1459,1419, 1336, 1130 cm⁻¹; MS (FAB) m/z 529 (M+H)

Example 2902-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenylamino-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.49-7.54 (m, 2H), 7.08-7.25 (m, 6H), 6.72 (t, 1H, J=7.2 Hz), 6.63 (d,2H, J=8.1 Hz), 6.21 (bt, 1H), 4.48 (d, 2H, J=5.7 Hz), 3.57 (q, 1H, J=6.9Hz), 3.35-3.46 (m, 3H), 3.01-3.04 (m, 5H), 2.60 (m, 2H), 2.17 (m, 2H),1.52 (d, 3H, J=6.9 Hz); IR (KBr) 2927. 1655. 1597. 1511. 1456. 1420.1375. 1334. 1155. 972. 756 cm⁻¹; MS (FAB) m/z 594(M+H)

Example 291N-(2-cyclohexyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48-7.54 (m, 2H), 7.38 (d, 1H, J=8.1 Hz), 7.14 (dd, 1H, J=11.1, 1.8 Hz)7.08 (d, 1H, J=8.1 Hz), 5.78 (bt, 1H), 4.49 (d, 2H, J=5.7 Hz), 3.57 (q,1H, J=6.9 Hz), 3.02 (s, 3H), 2.76 (m, 1H), 1.62-1.81 (m, 6H), 1.52 (d,3H, J=6.9 Hz), 1.25-1.31 (m, 4H); IR (KBr) 3300, 2927, 2855, 1643, 1512,1453, 1336, 1151, 973, 753 cm⁻¹; MS (FAB) m/z 502(M+H)

Example 2922-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

8.55 (s, 1H), 7.46-7.53 (m, 5H), 7.24-7.27 (m, 2H), 7.05 (dd, 1H,J=11.1, 1.8 Hz), 6.99 (d, 1H, J=8.1 Hz), 6.62 (bs 1H), 5.67 (bt, 1H),4.49 (d, 2H, J=5.7 Hz), 3.45 (q, 1H, J=6.9 Hz), 3.04 (s, 3H), 1.45 (d,3H, J=6.9 Hz); IR (neat) 3296, 2937, 1715, 1646, 1592, 1505, 1457, 1416,1361, 1277, 1159, 963, 758 cm⁻¹; MS (FAB) m/z 496(M+H)

Example 2932-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-thiopropionamide

¹H NMR (300 MHz, CDCl₃)

8.25 (bs, 1H), 7.48-7.54 (m, 2H), 7.10-7.25 (m, 3H), 4.93 (d, 2H, J=5.7Hz), 4.02 (q, 1H, J=6.9 Hz), 3.29 (m, 2H), 3.02 (s, 3H), 2.84 (m, 2H),1.70 (m, 2H), 1.67 (d, 3H, J=6.9 Hz), 1.50 (m, 1H), 1.24 (m, 2H), 0.98(d, 3H, J=6.6 Hz); IR (KBr) 3268, 2924, 1592, 1512, 1418, 1333, 1157,1045, 970, 833, 758 cm⁻¹; MS (FAB) m/z 533(M+H)

Example 296N-(2-azepan-1-yl-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methansulfonylamino-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.52 (dd, 1H, J=8.4, 8.4 Hz), 7.24 (d, 1H, J=7.7 Hz), 7.16 (dd, 1H,J=11.3, 2.0 Hz), 7.08 (d, 1H, J=8.8 Hz), 6.74 (d, 1H, J=7.7 Hz), 6.16(bs, 1H), 4.37 (m, 2H), 3.51 (q, 1H, J=7.1 Hz), 3.34-3.30 (m, 4H), 3.02(s, 3H), 1.80-1.60 (m, 4H), 1.58-1.49 (m, 4H), 1.51 (d, 3H, J=7.1 Hz),1.29 (s, 9H); IR (KBr) 3275, 2926, 1650, 1588, 1513, 1448, 1335 cm⁻¹; MS(FAB) m/z 505 (M+H)

Example 297N-(6-tert-butyl-2-dipropylamino-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.51 (dd, 1H, J=8.3, 8.3 Hz), 7.29 (d, 1H, J=7.7 Hz), 7.17 (dd, 1H,J=11.3 Hz, 1.8 Hz), 7.08 (d, 1H, J=8.4 Hz), 6.85 (d, 1H, J=7.7 Hz), 6.74(bs, 1H), 6.47 (bs, 1H), 4.47-4.33 (m, 2H), 3.49 (q, 1H, J=7.0 Hz),3.07-2.96 (m, 7H), 1.52-1.34 (m, 7H), 1.29 (s, 9H), 0.82 (t, 6H, J=7.4Hz); IR (KBr) 3290, 2961, 2871, 1650, 1513, 1456, 1335 cm⁻¹; MS (FAB)m/z 507 (M+H)

Example 298N-(2-but-2-enyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.59 (d, 1H, J=8.2 Hz), 7.52 (dd, 1H, J=8.3, 8.3 Hz), 7.20 (d, 1H, J=7.5Hz), 7.09 (dd, 1H, J=11.5, 1.8 Hz), 7.06 (d, 1H, J=9.1 Hz), 6.48 (bs,1H), 6.01 (bt, 1H), 5.76 (m, 1H), 5.58 (m, 1H), 4.94 (d, 2H, J=6.8 Hz),4.37 (d, 2H, J=6.0 Hz), 3.50 (q, 1H, J=7.0 Hz), 3.02 (s, 3H), 1.77 (d,3H, J=7.0 Hz), 1.48 (d, 3H, J=7.1 Hz); IR (neat) 3289, 2928, 1655, 1602,1512, 1462, 1422, 1373, 1334, 1265, 1156, 973, 904, 833 cm⁻¹; MS (FAB)m/z 490 (M+H)

Example 2992-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-2-enyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.59 (d, 1H, J=7.4 Hz), 7.51 (dd, 1H, J=8.4, 8.4 Hz), 7.20 (d, 1H, J=8.4Hz), 7.09 (dd, 1H, J=11.5, 1.8 Hz), 7.06 (d, 1H, J=9.2 Hz), 6.49 (s,1H), 6.01 (bt, 1H), 5.67 (m, 1H), 5.52 (m, 1H), 4.92 (d, 2H, J=4.7 Hz),4.37 (d, 2H, J=6.4 Hz), 3.50 (q, 1H, J=6.8 Hz), 3.03 (s, 3H), 2.20 (m,2H), 1.48 (d, 3H, J=7.1 Hz), 1.02 (t, 3H, J=7.5 Hz); IR (neat) 3292,2971, 1656, 1601, 1512, 1462, 1422, 1338, 1266, 1157, 977, 903, 759cm⁻¹; MS (FAB) m/z 504 (M+H)

Example 3002-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.62 (d, 1H, J=8.1 Hz), 7.53 (dd, 1H, J=8.3, 8.3 Hz), 7.45 (d, 1H, J=7.9Hz), 7.14 (dd, 1H, J=11.2, 2.0 Hz), 7.08 (d, 1H, J=8.4 Hz), 6.52 (bs,1H), 5.73 (bt, 1H), 6.41 (dt, 1H, J=11.6 Hz), 6.05 (m, 1H), 5.73 (bt,1H), 4.47 (m, 2H), 3.53 (q, 1H, J=7.1 Hz), 3.03 (s, 3H), 2.44 (m, 2H),1.51 (d, 3H, J=7.1 Hz), 1.47 (m, 2H), 0.92 (t, 3H, J=7.3 Hz); IR (neat)3296, 2927, 1652, 1513, 1458, 1339, 1280, 1156, 973 cm⁻¹; MS (FAB) m/z488 (M+H)

Example 3012-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.58 (d, 1H, J=7.9 Hz), 7.52 (dd, 1H, J=8.3, 8.3 Hz), 7.41 (d, 1H, J=7.9Hz), 7.15 (dd, 1H, J=11.2, 2.0 Hz), 7.08 (d, 1H, J=7.9 Hz), 6.51 (dt,2H, J=15.0 Hz), 5.64 (bt, 1H), 4.52 (m, 1H), 3.53 (q, 1H, J=7.4 Hz),3.03 (s, 3H), 2.24 (m, 2H), 1.59-1.45 (m, 5H), 0.97 (t, 3H, J=7.3 Hz);IR (neat) 3291, 2930, 1652, 1587, 1513, 1456, 1412, 1339, 1278, 1156,973, 936, 838 cm⁻¹; MS (FAB) m/z 488 (M+H)

Example 3022-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methyl-2-pentyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.50 (dd, 1H, J=8.3, 8.3 Hz), 7.13-7.01 (m, 3H), 6.03 (bt, 1H), 4.42 (m,2H), 4.29 (m, 2H), 3.45 (q, 1H, J=7.0 Hz), 3.02 (s, 3H), 2.49 (s, 3H),1.69 (m, 2H), 1.45 (d, 3H, J=7.1 Hz), 1.35 (m, 2H), 1.25 (m, 2H),0.98-0.87 (m, 5H); IR (neat) 3291, 2926, 1649, 1512, 1459, 1409, 1341,1291, 1245, 1158, 972, 912, 766 cm⁻¹; MS (FAB) m/z 520 (M+H)

Example 3032-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[2-(4-fluoro-phenyl)-ethyl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide

¹H NMR (300 MHz, CDCl₃)

7.35-7.56 (m, 3H), 7.02-7.17 (m, 4H), 6.88-6.97 (m, 2H), 6.54 (bs, 1H),5.49 (bt, 1H), 4.24-4.40 (m, 2H), 3.46 (q, 1H, J=7.0 Hz), 3.00-3.12 (m,7H), 1.49 (d, 3H, J=7.1 Hz); IR (KBr) 3296, 1652, 1511, 1456, 1338,1157, 972, 911, 832, 734 cm⁻¹; MS (FAB) m/z 542 (M+H)

Example 304N-(4-acetyl-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.44-7.53 (m, 2H), 7.27-7.43 (m, 5H), 7.21 (d, 1H, J=7.7 Hz), 7.11 (m,1H), 7.05 (d, 1H, J=8.6 Hz), 6.50 (bs, 1H), 6.12 (bt, 1H), 4.46 (d, 2H,J=5.7 Hz), 3.55 (q, 1H, J=7.0 Hz), 3.19-3.32 (m, 2H), 2.97-3.10 (m, 5H),2.41-2.54 (m, 2H), 2.05-2.20 (m, 2H), 1.95 (s, 3H), 1.52 (d, 3H, J=7.0Hz); IR (KBr) 2928, 1699, 1652, 1592, 1512, 1455, 1420, 1336, 1159, 965,910, 733 cm⁻¹; MS (FAB) m/z 621 (M+H)

Example 3072-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(phenyl-propionyl-amino)-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.42-7.52 (m, 6H), 7.05-7.19 (m, 4H), 6.99 (d, 1H, J=8.1 Hz), 6.16 (bt,1H), 4.75 (m, 1H), 4.36 (d, 2H, J=5.7 Hz), 4.12 (q, 2H, J=7.2 Hz), 3.48(q, 1H, J=6.9 Hz), 3.34 (m, 2H), 3.02 (s, 3H), 2.92 (m, 2H), 1.90 (m,2H), 1.46 (d, 3H, J=6.9 Hz), 1.25 (t, 3H, 7.2 Hz); IR (KBr) 2927, 1639,1592, 1509, 1456, 1414, 1373, 1337, 1275, 1158, 959, 705 cm⁻¹; MS (FAB)m/z 650(M+H)

Example 308N-[2-(4-dimethylamino-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.74 (d, 1H, J=7.8 Hz), 7.53 (dd, 1H, J=8.1, 8.1 Hz), 7.48 (d, 2H, J=8.7Hz), 7.31 (d, 1H, J=7.8 Hz), 7.02 (dd, 1H, J=11.1, 1.8 Hz), 6.97 (d, 1H,J=8.1 Hz), 6.72 (d, 1H, 8.7 Hz) (m, 6H), 6.58 (bs, 1H), 5.58 (bt, 1H),4.57 (d, 2H, J=5.7 Hz), 3.44 (q, 1H, J=6.9 Hz), 3.01 (s, 6H), 2.96 (s,3H), 1.44 (d, 3H, J=6.9 Hz); IR (KBr) 3291, 2926, 1658, 1611, 1514,1454, 1403, 1339, 1265, 1157, 972, 825, 736 cm⁻¹; MS (FAB) m/z 539(M+H)

Example 3092-[3-fluoro-4-(propan-2-sulfonylamino)-phenyl]-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.56 (dd, 1H, J=8.1, 8.1 Hz), 7.6 (d, 1H, J=7.5 Hz), 7.18 (d, 1H, J=7.5Hz), 7.07 (dd, 1H, J=11.1, 1.8 Hz), 7.05 (d, 1H, J=8.1 Hz), 6.56 (bs,1H), 6.33 (bt, 1H), 4.46 (d, 1H, J=5.7 Hz), 3.55 (q, 1H, J=6.9 Hz),3.20-3.34 (m, 3H), 2.81 (m, 2H), 1.71 (m, 3H), 1.50 (d, 3H, J=6.9 Hz),1.39 (d, 6H, J=6.9 Hz), 0.97 (d, 3H, J=6.3 Hz); IR (KBr) 3273, 2923,1657, 1592, 1511, 1458, 1419, 1332, 1270, 1142, 909, 732 cm⁻¹; MS (FAB)m/z 545 (M+H)

Example 3102-[3-fluoro-4-(2,2,2-trifluoro-ethansulfonylamino)-phenyl]-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48-7.53 (m, 2H), 7.21 (d, 1H, J=7.5 Hz), 7.16 (d, 1H, J=11.1 Hz), 7.09(d, 1H, J=8.1 Hz), 6.41 (bt, 1H), 4.48 (d, 2H, J=5.7 Hz), 3.84 (m, 2H),3.67 (q, 1H, J=6.9 Hz), 3.30 (m, 2H), 2.82 (m, 2H), 1.72 (m, 3H), 1.53(d, 3H, J=6.9 Hz), 1.25 (m, 2H), 0.98 (d, 3H, J=6.6 Hz); IR (neat) 2924,1657, 1592, 1512, 1456, 1418, 1358, 1253, 1169, 1134, 1086, 944 cm⁻¹; MS(FAB) m/z 585 (M+H)

Example 311N-[2-(2,6-dimethyl-morpholin-4-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48-7.52 (m, 2H), 7.10-7.25 (m, 3H), 6.52 (bs, 1H), 6.06 (bt, 1H), 4.47(d, 2H, J=5.7 Hz), 3.70 (m, 2H), 3.58 (q, 1H, J=6.9 Hz), 3.16 (m, 2H),3.04 (s, 3H), 2.64 (m, 2H), 1.55 (d, 3H, J=6.9 Hz), 1.19 (d, 6H, J=6.3Hz); IR (KBr) 3295, 2977, 1657, 1592, 1512, 1458, 1417, 1334, 1154,1006, 972, 912, 733 cm⁻¹; MS (FAB) m/z 533 (M+H)

Example 3122-(3-fluoro-4-trifluoromethylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.28-7.51 (m, 2H), 7.10-7.23 (m, 3H), 6.56 (bs, 1H), 6.06 (bt, 1H), 4.50(d, 2H, J=5.7 Hz), 3.57 (q, 1H, J=6.9 Hz), 3.33 (m, 2H), 2.84 (m, 2H),1.73 (m, 2H), 1.53 (d, 3H, J=6.9 Hz), 1.25 (m, 3H), 0.98 (d, 3H, J=6.0Hz); IR (neat) 2924, 1656, 1593, 1512, 1456, 1423, 1377, 1338, 1232,1203, 1142, 956, 738 cm⁻¹; MS (FAB) m/z 571 (M+H)

Example 3132-(3-fluoro-4-aminosulfonylamino-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.46-7.51 (m, 2H), 7.19 (d, 1H, J=7.2 Hz), 7.05-7.10 (m, 2H), 6.83 (bs,1H), 6.50 (bt, 1H), 5.04 (s, 2H), 4.46 (d, 2H, J=5.7 Hz), 3.57 (q, 1H,J=6.9 Hz), 3.27 (m, 2H), 2.81 (m, 2H), 1.78 (m, 2H), 1.51 (d, 3H, J=6.9Hz), 1.25 (m, 3H), 0.97 (d, 3H, J=6.0 Hz); IR (KBr) 3292, 2924, 1653,1592, 1514, 1455, 1418, 1339, 1169, 944, 833, 736 cm⁻¹; MS (FAB) m/z 571(M+H)

Example 314N-[2-(1,1-dioxo-1,6-thiomorpholin-4-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.50-7.56 (m, 2H), 7.33 (d, 1H, J=7.5 Hz), 7.09-7.17 (m, 2H), 5.94 (bt,1H), 4.46 (d, 2H, J=5.7 Hz), 3.72 (m, 4H), 3.60 (q, 1H, J=6.9 Hz), 3.16(m, 4H), 3.02 (s, 3H), 1.54 (d, 3H, J=6.9 Hz); IR (KBr) 3369, 2933,1659, 1590, 1514, 1462, 1415, 1333, 1278, 1124, 974, 912, 732 cm⁻¹; MS(FAB) m/z 553 (M+H)

Example 315N-(6′-difluoromethyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47-7.54 (m, 2H), 7.06-7.19 (m, 3H), 6.48 (t, 1H, J=55.0 Hz), 6.41 (bs,1H), 6.06 (bt, 1H), 4.46 (d, 2H, J=5.7 Hz), 3.55 (q, 1H, J=6.9 Hz), 3.25(m, 2H), 3.02 (s, 3H), 2.79 (m, 2H), 1.71 (m, 2H), 1.52 (d, 3H, J=6.9Hz), 1.25 (m, 3H), 0.97 (d, 6H, J=6.0 Hz); IR (KBr) 3291, 2922, 1652,1589, 1512, 1421, 1334, 1158, 1087, 1041, 970, 795 cm⁻¹; MS (FAB) m/z499 (M+H)

Example 316N-(4,6′-dimethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.50 (dd, 1H, J=8.1, 8.1 Hz), 7.28 (d, 1H, J=7.5 Hz), 7.13 (dd, 1H,J=8.1, 1.8 Hz), 7.07 (d, 1H, J=8.1 Hz), 6.75 (d, 1H, J=7.5 Hz), 6.72(bs, 1H), 6.46 (bt, 1H), 4.40 (d, 2H, J=5.7 Hz), 3.51 (q, 1H, J=6.9 Hz),3.18 (m, 2H), 3.02 (s, 3H), 2.77 (m, 2H), 2.42 (s, 3H), 1.72 (m, 2H),1.50 (d, 3H, J=6.9 Hz), 1.26 (m, 3H), 0.97 (d, 6H, J=6.0 Hz); IR (KBr)3289, 2922, 1651, 1584, 1511, 1453, 1374, 1333, 1157, 1115, 971, 735cm⁻¹; MS (FAB) m/z 463(M+H)

Example 3172-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.21-7.54 (m, 7H), 7.02-7.16 (m, 3H), 6.63 (bs, 1H), 6.35 (bt, 1H), 6.18(m, 1H), 4.52 (d, 2H, J=5.7 Hz), 3.87 (d, 2H, J=2.7 Hz), 3.36-3.59 (m,3H), 2.99 (s, 3H), 2.67 (m, 2H), 1.52 (d, 3H, J=6.9 Hz)

IR (KBr) 3293, 2930, 1656, 1592, 1512, 1421, 1336, 1274, 1229, 1157,970, 833, 755, 697 cm⁻¹; MS (FAB) m/z 577(M+H)

Example 318N-(4,4′-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.48 (dd, 1H, J=8.1, 8.1 Hz), 7.14 (s, 1H), 7.02-7.07 (m, 2H), 6.80 (bs,1H), 4.52 (d, 2H, J=5.7 Hz), 3.48 (q, 1H, J=6.9 Hz), 3.17 (m, 1H),2.01-3.04 (m, 4H), 2.79 (m, 2H), 2.38 (m, 2H), 1.70 (m, 2H), 1.47 (d,3H, J=6.9 Hz), 1.13-1.25 (m, 3H), 0.97 (d, 3H, J=6.3 Hz); IR (KBr) 3302,2923, 1644, 1512, 1451, 1408, 1333, 1280, 1159, 975, 759 cm⁻¹; MS (FAB)m/z 531(M+H)

Example 319N-[2-(4-cyclohexyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.52 (t, 1H, J=8.2 Hz), 7.31 (s, 1H),7.26˜7.28 (m, 2H), 7.08˜7.16 (m, 2H), 6.42 (bs, 1H), 4.52 (d, 2H,J=5.9), 3.54 (q, 1H, J=7.1 Hz), 3.0 (s, 3H), 2.88˜2.95 (m, 4H), 2.67 (s,3H), 1.81˜1.90 (m, 3H), 1.64 (m, 2H), 1.52 (d, 3H, J=7.0 Hz), 1.20˜1.30(m, 5H), 0.89˜0.92 (m, 2H); IR (KBr) 3294, 2855, 1654, 1509, 1424, 975,910, 734 cm⁻¹; MS (FAB) m/z 585 (M+H)

Example 320N-(4′-tert-butyl-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.28˜7.55 (m, 6H), 7.16 (d, 2H, J=7.4 Hz),7.07 (dd, 1H, J=11.2, 1.8 Hz), 6.97˜7.02 (m, 1H), 5.51 (bt, 1H),4.41˜4.51 (m, 2H), 3.43 (q, 1H, J=7.1 Hz), 3.0 (s, 3H), 1.44 (d, 3H,J=7.1 Hz), 1.36 (s, 9H); IR (KBr) 2965, 1460, 1259, 1078, 979, 908, 836,734 cm⁻¹; MS (FAB) m/z 551(M+H)

Example 3212-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4′-methoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.46˜7.54 (m, 3H), 7.39 (d, 1H, J=8.0 Hz),7.14 (dd, 2H, J=6.4, 2.0 Hz), 7.05 (dd, 1H, J=11.0, 1.8 Hz), 6.99 (d,1H, J=8.3 Hz), 6.93 (dd, 2H, J=6.8, 2.2 Hz), 5.46 (bt, 1H), 4.43 (t, 2H,J=3.7 Hz), 3.86 (s, 3H), 3.43 (q, 1H, J=7.5 Hz), 3.02 (s, 3H), 1.44 (d,3H, J=7.0 Hz); IR (KBr) 3295, 1422, 1252, 1042, 973, 907, 835, 732 cm⁻¹;MS (FAB) m/z 525(M+H)

Example 322N-(3′-chloro-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.58˜7.32 (m, 6H), 7.23 (m, 1H), 7.14˜7.00 (m,3H), 5.61 (b t, 1H), 4.39 (t, 2H, J=5.5 Hz), 3.46 (q, 1H, J=7.1 Hz), 3.0(s, 3H), 1.45 (d, 3H, J=7.1 Hz); IR (KBr) 3290, 1651, 1421, 1078, 1041,974, 908, 732 cm⁻¹; MS (FAB) m/z 528 (M+H)

Example 3232-(3-fluoro-4-methylsulfonamido-phenyl)-N-(3′-fluoro-5-trifluoromethyl-biphenyl-2-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.38˜7.59 (m, 5H), 7.00˜7.09 (m, 4H), 6.93 (d,1H, J=10.4 Hz) 4.39 (m, 2H), 3.45 (q, 1H, J=7.3 Hz), 3.03 (s, 3H), 1.46(d, 3H, J=7.1 Hz); IR (KBr) 3289, 1586, 1446, 1277, 1078, 973, 907, 733cm⁻¹; MS (FAB) m/z 513 (M+H)

Example 324N-(3′-chloro-4′-fluoro-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.49˜7.59 (m, 2H), 7.37˜7.44 (m, 2H),7.02˜7.22 (m, 5H), 5.54 (bt, 1H), 4.38 (d, 2H, J=6.0 Hz), 3.49 (q, 1H,J=7.0 Hz), 3.04 (s, 3H), 1.47 (d, 3H, J=7.1 Hz); IR (KBr) 3246, 1420,1265, 1077, 973, 908, 828, 732 cm⁻¹; MS (FAB) m/z 548 (M+H)

Example 325N-(3′,4′-dimethoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.43˜7.53 (m, 3H), 7.38 (d, 1H, J=8.1 Hz),7.07 (dd, 1H, J=11.3, 2.0 Hz), 7.0 (d, 1H, J=8.2 Hz), 6.90 (d, 1H, J=8.2Hz), 6.74˜6.77 (m, 2H), 5.72 (bs, 1H), 4.44 (m, 2H), 3.92 (s, 3H), 3.86(s, 3H), 3.46 (q, 1H, J=7.1 Hz), 3.01 (s, 3H), 1.44 (d, 3H, J=7.1 Hz);IR (KBr) 2936, 1423, 1078, 1025, 974, 908, 765, 732 cm⁻¹; MS (FAB) m/z555 (M+H)

Example 326N-[2-(3,4-dimethoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.76 (d, 1H, J=8.1 Hz), 7.57 (d, 1H, J=8.0Hz), 7.45 (t, 1H, J=8.3 Hz), 6.79˜7.08 (m, 5H), 5.90 (bt, 1H), 4.53 (d,2H, J=5.5 Hz), 3.91 (s, 3H), 3.88 (s, 3H), 3.49 (q, 1H, J=6.9 Hz), 3.02(s, 3H), 1.43 (d, 3H, J=7.2 Hz); IR (KBr) 3271, 2937, 1587, 1416, 1025,972, 913 cm⁻¹; MS (FAB) m/z 556 (M+H)

Example 3274-(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-yloxymethyl)-piperidine-1-carbonicacid tert-butyl ester

¹H NMR (CDCl₃) δ 7.60 d, 1H, J=7.5 Hz), 7.52 (dd, 1H, J=8.4, 8.4 Hz),7.21 (d, 1H, J=7.5 Hz), 7.12-7.05 (m, 2H), 5.83 (bs, NH), 4.37 (d, 2H,J=5.9 Hz), 4.25-4.07 (m, 4H), 3.53 (q, 1H, J=6.4 Hz), 3.04 (s, 3H),2.78-2.63 (m, 2H), 1.90 (m, 1H), 1.68-1.55 (m, 2H), 1.48 (s, 9H),1.25-1.05 (m, 2H); IR (neat) 3303, 2935, 1665, 1426, 1359, 1271, 1157,757 cm⁻¹; MS (FAB) m/z 633 (M+H)

Example 331N-(2-dipropylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.36-7.41 (m, 2H), 7.08-7.18 (m, 4H), 6.29 (bt, 1H), 4.42 (d, 2H, J=5.7Hz), 3.56 (q, 1H, J=6.9 Hz), 3.09 (t, 4H, J=7.5 Hz), 2.99 (s, 3H), 2.32(s, 3H), 2.82 (m, 2H), 1.52 (d, 3H, J=6.9 Hz), 1.43 (m, 4H), 0.82 (t,6H, J=7.5 Hz); IR (neat) 3272, 2965, 1655, 1594, 1503, 1460, 1419, 1331,1152, 1027, 895, 825, 762 cm⁻¹; MS (FAB) m/z 563 (M+H)

Example 3392-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6-trifluoromethyl-2-(4-trifluoromethyl-cyclohexyloxy)-pyridin-3-ylmethyl]-propionamide

¹H NMR (CDCl₃) δ 7.59 (d, 1H, J=7.0 Hz), 7.51 (dd, 1H, J=8.2, 8.2 Hz),7.20 (d, 1H, J=7.5 Hz), 7.13-7.05 (m, 2H), 6.50 (bs, NH), 5.91 (bt, NH),5.43 (m, 1H), 4.39 (m, 2H), 3.51 (q, 1H, J=6.6 Hz), 3.03 (s, 3H),2.20-2.08 (m, 3H), 1.85-1.77 (m, 2H), 1.63-1.50 (m, 4H), 1.49 (d, 3H,J=7.1 Hz); IR (neat) 3293, 2953, 1658, 1513, 1422, 1343, 1264, 1141, 970cm⁻¹; MS (FAB) m/z 586 (M+H)

Example 3402-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6-trifluoromethyl-2-(4-trifluoromethyl-cyclohexyloxy)-pyridin-3-ylmethyl]-propionamide

¹H NMR (CDCl₃) δ 7.57-7.50 (m, 2H), 7.19 (d, 1H, J=7.3 Hz), 7.13-7.06(m, 2H), 5.90 (bt, NH), 5.03 (m, 1H), 4.36 (m, 2H), 3.53 (q, 1H, J=7.4Hz), 3.05 (s, 3H), 2.28-2.00 (m, 4H), 1.62-1.25 (m, 5H), 1.50 (d, 3H,J=7.1 Hz); IR (neat) 3288, 2952, 1658, 1512, 1422, 1365, 1338, 1275,1156, 975 cm⁻¹; MS (FAB) m/z 586 (M+H)

Example 3414-(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-yloxy)-piperidine-1-carbonicacid tert-butyl ester

¹H NMR (CDCl₃) δ 7.60 (d, 1H, J=7.3 Hz), 7.50 (dd, 1H, J=8.2, 8.2 Hz),7.20 (d, 1H, J=7.3 Hz), 7.13-7.04 (m, 2H), 5.87 (bt, NH), 5.24 (m, 1H),4.36 (d, 2H), 3.70-3.62 (m, 2H), 3.54 (q, 1H, J=7.7 Hz), 3.28-3.17 (m,2H), 3.04 (s, 3H), 1.98-1.88 (m, 2H), 1.54-1.40 (m, 2H), 1.51 (d, 3H),1.50 (s, 9H); IR (neat) 3301, 2977, 1665, 1420, 1337, 1276, 1163, 1027cm⁻¹; MS (FAB) m/z 619 (M+H)

Example 3424-[(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-ylamino)-methyl]-piperidine-1-carbonicacid tert-butyl ester

¹H NMR (CDCl₃) δ 7.48 (dd, 1H, J=8.2, 8.2 Hz), 7.25 (d, 1H), 7.16 (d,1H), 7.06 (d, 1H), 6.77 (d, 1H, J=7.3 Hz), 6.21 (bs, NH), 5.93 (bs, NH),4.32 (m, 2H), 4.06 (m, 2H), 3.49 (q, 1H, J=7.3 Hz), 3.32 (m, 2H), 2.66(m, 2H), 1.76 (m, 2H), 1.51 (d, 3H, J=7.0 Hz), 1.46 (s, 9H); IR (neat)3303, 2927, 1658, 1611, 1515, 1428, 1335, 1161, 734 cm⁻¹; MS (FAB) m/z632 (M+H)

Example 3432-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(piperidin-4-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (CDCl₃) δ 7.58 (d, 1H, J=7.9 Hz), 7.43 (dd, 1H, J=8.3, 8.3 Hz),7.29 (d, 1H, J=7.4 Hz), 7.22-7.15 (m, 2H), 4.47-4.23 (m, 4H), 3.73 (q,1H, J=7.1 Hz), 3.43-3.36 (m, 2H), 3.05-2.93 (m, 2H), 3.00 (s, 3H),2.04-1.96 (m, 3H), 1.53-1.45 (m, 2H), 1.46 (d, 3H, J=7.1 Hz); IR (neat)3405, 2923, 1674, 1512, 1425, 1334, 1270, 1153 cm⁻¹; MS (FAB) m/z 533(M+H)

Example 3442-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(piperidin-4-yloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (CDCl₃) δ 7.58 (d, 1H, J=7.5 Hz), 7.41 (dd, 1H, J=8.3, 8.3 Hz),7.27 (d, 1H, J=7.5 Hz), 7.19-7.11 (m, 2H), 5.29 (m, 1H), 4.36 (m, 2H),3.71 (q, 1H, J=7.0 Hz), 3.20 (m, 2H), 3.01-2.90 (m, 2H), 2.97 (s, 3H),2.06 (m, 2H), 1.81 (m, 2H), 1.45 (d, 3H, J=7.1 Hz); IR (neat) 3397,2923, 1657, 1505, 1421, 1292, 1115, 987 cm⁻¹; MS (FAB) m/z 519 (M+H)

Example 3452-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-p-tolyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.74 (J=7.5 Hz), 7.47 (dd, 1H, J=8.4, 8.4 Hz),7.31 (d, 1H, J=7.9 Hz), 7.18 (d, 2H, J=8.8 Hz), 7.01 (m, 2H), 6.91 (m,2H), 4.49 (m, 2H), 3.58 (q, 1H, J=7.0 Hz), 2.94 (s, 3H), 1.49 (d, 3H,J=7.1 Hz); IR (neat) 3292, 1655, 1593, 1509, 1465, 1406, 1336, 1260,1156, 972, 940, 831 cm⁻¹; MS (FAB) m/z 526 (M+H)

Example 346N-[2-(2-cyclohexyl-vinyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.57 (d, 1H, J=7.9 Hz), 7.52 (dd, 1H, J=8.3, 8.3 Hz), 7.41 (d, 1H, J=7.9Hz), 7.15 (dd, 1H, J=11.3, 2.0 Hz), 7.08 (d, 1H, J=7.0 Hz), 6.49 (m,2H), 5.64 (bt, 1H), 4.52 (m, 2H), 3.53 (q, 1H, J=7.0 Hz), 3.03 (s, 3H),2.17 (m, 1H), 1.85-1.73 (m, 4H), 1.52 (d, 3H, J=7.1 Hz), 1.34-1.23 (m,6H); IR (neat) 3292, 2927, 2853, 1651, 1588, 1513, 1452, 1412, 1340,1157, 973, 843 cm⁻¹; MS (FAB) m/z 528 (M+H)

Example 3472-(3-fluoro-4-methylsulfonamiclo-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-butyramide

¹H NMR (300 MHz, CDCl₃)

7.51 (dd, 1H, J=8.3, 8.3 Hz), 7.49 (d, 1H, J=8.3 Hz), 7.18 (m, 2H), 7.08(d, 1H, J=8.3 Hz), 6.51 (bs, 1H), 6.34 (bt, 1H), 4.47 (m, 2H), 3.31 (m,2H), 3.21 (t, 1H, J=7.7 Hz), 3.03 (s, 3H), 2.83 (m, 2H), 2.16 (m, 1H),1.80 (m, 1H), 1.73 (m, 2H), 1.55 (m, 1H), 1.26 (m, 2H), 0.98 (d, 3H,J=6.6 Hz), 0.91 (t, 3H, J=7.5 Hz); IR (neat) 3291, 2925, 1652, 1592,1512, 1456, 1419, 1335, 1272, 1157, 969, 832 cm⁻¹; MS (FAB) m/z 531(M+H)

Example 348N-[2-(3,5-dimethoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.81 (d, 1H, J=8.0 Hz), 7.61 (d, 1H, J=8.0Hz), 7.49 (t, 1H, J=8.4 Hz), 6.98-7.07 (m, 2H), 6.51 (s, 3H), 5.64 (bt,1H), 4.49 (d, 2H, J=3.8 Hz), 3.81 (s, 6H), 3.46 (q, 1H, J=7.1 Hz), 3.03(s, 3H), 1.45 (d, 3H, J=7.1 Hz); IR (KBr) 3293, 2931, 1655, 1458, 1402,973, 911, 732 cm⁻¹; MS (FAB) m/z 556 (M+H)

Example 349N-(2-cyclopentyloxy-4-methyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide)

¹H NMR (300 MHz, CDCl₃) δ 7.49 (m, 1H), 7.00˜7.07 (m, 3H), 6.05 (bt,1H), 5.43 (m, 1H), 4.39 (m, 2H), 3.47 (q, 1H, J=7.1 Hz), 3.02 (s, 3H),2.47 (s, 3H), 1.96 (m, 2H), 1.58˜1.65 (m, 6H), 1.45 (d, 3H, J=7.1 Hz);IR (KBr) 3271, 2967, 1290, 1246, 1093, 973, 911, 731 cm⁻¹; MS (FAB) m/z518 (M+H)

Example 350N-(3′,5′-dimethoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.40˜7.56 (m, 4H), 6.98˜7.08 (m, 2H), 6.48 (t,1H, J=2.4 Hz), 6.35 (d, 2H, J=2.2 Hz), 5.56 (bt, 1H), 4.43 (t, 2H, J=5.5Hz), 3.81 (s, 6H), 3.43 (q, 1H, J=7.2 Hz), 3.02 (s, 3H), 1.44 (d, 3H,J=7.1 Hz); IR (KBr) 3298, 1651, 1512, 1455, 1207, 1078, 907 cm⁻¹; MS(FAB) m/z 555 (M+H)

Example 3515-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-4-(4-methyl-piperidin-1-yl)-2-trifluoromethyl-benzoicacid ethyl ester

¹H NMR (300 MHz, CDCl₃) δ 7.74 (s, 1H), 7.48 (t, 1H, J=8.4 Hz),7.11˜7.20 (m, 2H), 4.38˜4.31 (m, 4H), 3.68˜3.59 (m, 3H), 3.02 (s, 3H),2.83˜2.92 (m, 2H), 1.74˜1.52 (m, 3H), 1.53 (d, 3H, J=7.1 Hz), 1.36 (t,3H, J=7.1 Hz), 1.29˜1.26 (m, 2H), 0.97 (d, 3H, J=6.4 Hz); IR (KBr) 3364,2927, 1725, 1373, 1031, 916, 796, 732 cm⁻¹; MS (FAB) m/z 589 (M+H)

Example 352N-[2-(1-butyl-pentyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.49˜7.56 (m, 2H), 7.15 (d, 1H, J=7.7 Hz),7.08 (t, 1H, J=5.9 Hz), 6.47 (bs, 1H), 5.98 (bt, 1H), 5.29 (m, 1H), 4.37(m, 2H), 3.49 (q, 1H, J=7.0 Hz), 3.03 (s, 3H), 1.57 (m, 2H), 1.49 (d,3H, J=7.0 Hz), 1.24˜1.31 (m, 8H), 0.88˜0.90 (m, 6H); IR (neat) 3295,2933, 2865, 1601, 1513, 1463, 1269, 974 cm⁻¹; MS (FAB) m/z 562(M+H)

Example 353N-(6-tert-butyl-2-isobutoxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.49 (t, 1H, J=8.4 Hz), 7.36 (d, 1H, J=7.5Hz), 7.04˜7.15 (m, 2H), 6.79 (d, 1H, J=7.5 Hz), 6.06 (bt, 1H), 4.32 (m,2H), 4.05˜4.16 (m, 3H), 3.48 (q, 1H, J=7.1 Hz), 3.02 (s, 3H), 1.48 (d,3H, J=7.1 Hz), 1.29 (s, 9H), 0.97 (d, 6H, J=6.6 Hz); IR (KBr) 3291,1585, 1410, 1254, 1119, 1019, 972, 732 cm⁻¹; MS (FAB) m/z 480 (M+H)

Example 3542-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenylethynyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.80 (d, 1H, J=8.0 Hz), 7.58 (d, 1H, J=8.1 Hz), 7.49-7.55 (m, 2H),7.35-7.48 (m, 4H), 7.00-7.11 (m, 2H), 6.08 (bt, 1H), 4.65 (d, 2H, J=6.0Hz), 3.56 (q, 1H, J=7.0 Hz), 3.00 (s, 3H), 1.49 (d, 3H, J=7.1 Hz); IR(KBr) 3297, 2220, 1657, 1513, 1454, 1405, 1340, 1153, 1115, 972, 912,759, 731 cm⁻¹; MS (FAB) m/z 520 (M+H)

Example 3552-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methoxy-propoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide(SJS-284)

¹H NMR (300 MHz, CDCl₃)

7.61 (d, 1H, J=7.3 Hz), 7.49 (dd, 1H, J=8.1, 8.1 Hz), 7.20 (d, 1H, J=7.3Hz), 7.02-7.11 (m, 2H), 6.44 (bt, 1H), 4.47-4.50 (m, 2H), 4.34 (d, 2H,J=6.0 Hz), 3.42-3.61 (m, 3H), 3.36 (s, 3H), 3.03 (s, 3H), 1.89-2.01 (m,2H), 1.47 (d, 3H, J=7.1 Hz); IR (KBr) 3296, 2924, 1656, 1603, 1513,1425, 1338, 1269, 1157, 975, 908 cm⁻¹; MS (FAB) m/z (M+H)

Example 356N-(4-benzyl-4′-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.49 (dd, 1H, J=8.3, 8.3 Hz), 7.27-7.35 (m, 2H), 7.11-7.25 (m, 4H),6.89-7.10 (m, 2H), 6.70 (bt, 1H), 4.42-4.58 (m, 2H), 3.45 (q, 1H, J=7.1Hz), 3.02-3.21 (m, 2H), 2.99 (s, 3H), 2.68-2.83 (m, 2H), 2.58 (d, 2H,J=6.6 Hz), 2.37 (s, 3H), 1.64-1.80 (m, 3H), 1.47 (d, 3H, J=7.1 Hz),1.18-1.32 (m, 2H)

Example 3572-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methylene-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (CDCl₃) δ 7.53-7.48 (m, 2H), 7.22 (d, 1H, J=7.7 Hz), 7.16-7.08(m, 2H), 6.52 (bs, NH), 6.19 (bt, NH), 4.76 (s, 2H), 4.50 (d, 2H, J=5.7Hz), 3.57 (q, 1H, J=7.0 Hz), 3.13 (m, 4H), 3.03 (s, 3H), 2.30 (m, 4H),1.54 (d, 3H, J=7.1 Hz); IR (neat) 3293, 2931, 1720, 1657, 1593, 1513,1458, 1419, 1335, 1158 cm⁻¹; MS (FAB) m/z 515 (M+H)

Example 358N-[2-(6-aza-spiro[2.5]oct-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (CDCl₃) δ 7.55-7.49 (m, 2H), 7.22 (d, 1H, J=7.7 Hz), 7.17-7.08(m, 2H), 6.52 (bs, NH), 6.35 (bt, NH), 4.50 (d, 2H, J=5.7 Hz), 3.56 (q,1H), 3.12 (m, 4H), 3.03 (s, 3H), 1.53 (d, 3H, J=7.1 Hz), 1.45 (m, 4H),0.35 (s, 4H); IR (neat) 3292, 2926, 1656, 1593, 1513, 1420, 1335, 1158,734 cm⁻¹; MS (FAB) m/z 529 (M+H)

Example 3592-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methyl-but-2-enyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (CDCl₃) δ 7.58 (d, 1H, J=7.3 Hz), 7.51 (m, 1H), 7.18 (d, 1H,J=7.5 Hz), 7.12-7.05 (m, 2H), 6.07 (bt, NH), 5.38 (m, 1H), 4.87 (m, 2H),4.37 (m, 2H), 3.51 (q, 1H, J=7.1 Hz), 3.03 (s, 3H), 1.78 (s, 6H), 1.48(d, 3H, J=7.1 Hz); IR (neat) 3289, 2935, 1656, 1603, 1513, 1420, 1333,1262, 1158, 977 cm⁻¹; MS (FAB) m/z 503 (M+H)

Example 360N-[2-(3-cyclohexyl-propyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.50-7.57 (m, 2H), 7.44 (d, 1H, J=7.9 Hz),7.17 (dd, 1H, J=11.0, 2.0 Hz), 7.10 (d, 1H, J=8.3 Hz), 6.47 (bs, 1H),5.69 (bt, 1H), 4.40-4.57 (m, 2H), 3.57 (q, 1H, J=7.1 Hz), 3.05 (bs, 3H),2.75 (t, 2H, J=7.7 Hz), 1.60-1.74 (m, 8H), 1.53 (d, 3H, J=7.1 Hz),1.09-1.30 (m, 5H), 0.79-0.91 (m, 2H); IR (KBr) 3292, 2924, 2851, 1654,1512, 1454, 1408, 1340, 1278, 1158, 972, 909, 733 cm⁻¹; MS (FAB) m/z 544(M+H)

Example 361N-[2-(3-ethoxy-propoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃) δ 7.61 (d, 1H, J=7.5 Hz) 7.50 (dd, 1H, J=8.3,8.3 Hz), 7.20 (d, 1H, J=7.5 Hz), 7.01-7.12 (m, 2H), 6.35 (bt, 1H),4.37-4.50 (m, 2H), 4.35 (d, 2H, J=6.0 Hz), 3.47-3.60 (m, 5H), 3.03 (s,3H), 1.90-2.01 (m, 2H), 1.47 (d, 3H, J=7.0 Hz), 1.20 (t, 3H, J=7.1 Hz);IR (KBr) 3296, 2923, 1657, 1512, 1425, 1338, 1269, 1157, 972 cm⁻¹; MS(FAB) m/z (M+H)

Example 3622-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-phenoxy-ethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide

¹H NMR (300 MHz, CDCl₃)

7.66 (d, 1H, J=7.3 Hz), 7.41 (dd, 1H, J=8.4, 8.4 Hz), 7.22-7.35 (m, 3H),6.88-7.05 (m, 5H), 6.42 (bs, 1H), 6.21 (bt, 1H), 4.63-4.82 (m, 2H),4.27-4.42 (m, 4H), 3.34 (q, 1H, J=7.1 Hz), 2.99 (s, 3H), 1.38 (d, 3H,J=7.0 Hz); IR (KBr) 3295, 2924, 1657, 1598, 1510, 1423, 1339, 1244,1157, 967, 910, 756 cm⁻¹; MS (FAB) m/z (M+H)

Example 363N-[2-(3,5-dimethoxy-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.63 (d, 1H, J=7.3 Hz) 7.45 (dd, 1H, J=8.3, 8.3 Hz), 7.24 (d, 1H, J=7.5Hz), 7.04 (dd, 1H, J=11.2, 2.0 Hz), 6.98 (d, 1H, J=8.8 Hz), 6.59 (d, 2H,J=2.2 Hz), 6.45 (t, 1H, J=2.4 Hz), 6.00 (bt, 1H), 5.26-5.41 (m, 2H),4.30-4.48 (m, 2H), 3.81 (s, 6H), 3.43 (q, 1H, J=7.3 Hz), 3.01 (s, 3H),1.43 (d, 3H, J=7.1 Hz); IR (KBr) 1656, 1601, 1512, 1463, 1419, 1353,1156, 1068, 976, 835 cm⁻¹; MS (FAB) m/z (M+H)

Example 3642-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-hydroxymethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.54 (d, 1H, J=8.3 Hz), 7.51 (d, 1H, J=8.3 Hz), 7.23 (d, 1H, J=7.7 Hz),7.16-7.08 (m, 2H), 6.24 (bs, 1H), 4.48 (m, 2H), 3.57-3.54 (m, 3H), 3.28(m, 2H), 3.05 (s, 3H), 2.85 (m, 2H), 1.80 (m, 1H), 1.57-1.51 (m, 5H),1.29 (m, 2H); IR (KBr) 3294, 2925, 1655, 1593, 1513, 1419, 1334 cm⁻¹; MS(FAB) m/z 533 (M+H)

Example 365N-(6′-tert-butyl-4-phenyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47 (dd, 1H, J=8.3, 8.3 Hz), 7.37-7.14 (m, 7H), 7.09 (d, 1H, J=8.6 Hz),6.92 (d, 1H, J=7.7 Hz), 6.72 (bs, 1H), 4.47 (m, 2H), 3.55 (q, 1H, J=7.1Hz), 3.40 (m, 2H), 3.01-2.89 (m, 5H), 2.68 (m, 1H), 1.93-1.68 (m, 4H),1.52 (d, 3H, J=7.1 Hz), 1.32 (s, 9H); IR (KBr) 3289, 2958, 1651, 1512,1449, 1401, 1335 cm⁻¹; MS (FAB) m/z 567 (M+H)

Example 366N-{6-tert-butyl-2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.47 (dd, 1H, J=8.2, 8.2 Hz), 7.34 (d, 1H, J=7.9 Hz), 7.17-6.87 (m, 7H),6.51 (bs, 1H), 4.47 (m, 2H), 3.53 (q, 1H, J=6.9 Hz), 3.20-3.10 (m, 8H),2.98 (s, 3H), 1.51 (d, 3H, J=6.9 Hz), 1.30 (s, 9H); IR (KBr) 3291, 2961,1562, 1510, 1449, 1400, 1335 cm⁻¹; MS (FAB) m/z 586 (M+H)

Example 3672-(4-methylsulfonamido-3-methyl-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide

¹H NMR (300 MHz, CDCl₃)

7.74 (d, 1H, J=8.1 Hz), 7.39 (d, 1H, J=7.8 Hz), 7.35 (d, 1H, J=7.8 Hz),7.32 (d, 1H, J=7.8 Hz), 7.12-7.14 (m, 2H), 6.92 (d, 1H, J=7.5 Hz), 6.26(s, 1H), 5.68 (bs, 1H), 4.45 (d, 2H, J=5.7 Hz), 3.53 (q, 1H, J=7.2 Hz),3.41 (m, 4H), 3.05 (s, 3H), 2.32 (s, 3H), 1.85 (m, 4H), 1.50 (d, 3H,J=7.2 Hz); IR (KBr) 3292, 2926, 1651, 1599, 1537, 1458, 1330, 1153 cm⁻¹;MS (FAB) m/z 485 (M+H)

 83(S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-propionamide  84(R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-propionamide  93(S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide  94(R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide  96(S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide  97(R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide  982-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-4-trifluoromethyl-benzyl)-propionamide  99(R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-4-trifluoromethyl-benzyl)-propionamide 1112-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-propoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 116N-(2-butylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 120(S)-N-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 121(R)-N-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 1232-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 133N-(4-tert-butyl-2-isobutoxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide1342-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 140N-[2-butoxy-6-(chlor-difluor-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 144(S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 145(R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 1912-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-styryl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide 1922-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenethyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 193N-{2-[4-(3-chloro-pyridin-2-yl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 194N-{2-[4-(3-chloro-pyridin-2-yl)-2-methyl-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 2132-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(3-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-pyridin-3-ylmethyl}-propionamide 2142-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-pyridin-2-yl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 2152-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide239(R)-N-(2-cyclohexyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 242N-[2-(4-ethyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 250N-[2-(3,4-dichloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 251N-[2-(3-tert-butyl-1-oxa-2,8-diaza-spiro[4.5]dec-2-en-8-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 2522-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-phenyl-1-oxa-2,8-diaza-spiro[4.5]dec-2-en-8-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 2532-(3-fluoro-4-(pentafluorsulfanylsulfonamido)phenyl)-N-p-tolylpropanamide2542-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-fluoro-4-methoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 265N-[2-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 266N-(2-benzo[1,3]dioxol-5-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 2722-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methylsulfonamido-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 2732-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-methyl-propenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 274N-[2-(3,3-dimethyl-but-1-enyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 2752-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1H-indol-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 2762-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1H-indol-5-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 277N-[2-(4-chloro-3-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 2782-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-3-methyl-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 294N-(2-cyclohexylsulfanyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 2952-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 328N-(6-tert-butyl-2-pentyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 329N-[6-tert-butyl-2-(3-methyl-butoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 330N-(4-dimethylamino-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 3322-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide 334N-(2-cyclohex-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 335N-[2-(1-ethyl-propoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 3362-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1-propyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 3372-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1-isobutyl-3-methyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 338N-[2-(4,4-dimethyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide [368]N-((2-(1H-indol-4-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [369]N-((6-tert-butyl-2-propoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [370]N-((6-tert-butyl-2-(3-methoxypropoxy)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [371]N-((6-tert-butyl-2-(4-(dimethylamino)-4-phenylpiperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [372]N-((6-tert-butyl-2-methoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [373]N-((6-tert-butyl-2-ethoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [374]N-((6-tert-butyl-2-isopropoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [375]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pentyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide, [376]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(hexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide, [377]N-((2-(3,5-dimethylcyclohexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [378]N-((6-tert-butyl-2-(2-ethoxyethoxy)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide,

Pharmacological Data

The affinity of the compounds according to the invention for thevanilloid receptor 1 (VR1/TRPV1 receptor) was determined as describedabove (pharmacological methods I or II).

The compounds according to the invention of the above-stated formula Iexhibit excellent affinity for the VR1/TRPV1 receptor (table 2).

TABLE 2 Compound IC₅₀ (human) according to K_(i) (rat) K_(i) (human)[nM] Example [nM] [nM] after pH stimulus 1 684 387 2 3.5 0.4 218 3 2.61.7 135 6 95 169 2613 10 1.1 0.3 64 11 1.1 0.3 46.7 12 4.3 1.3 169 133.8 0.6 211 18 47 68.9 2711 19 1.0 0.3 31 20 5.4 2.1 93 21 1.3 0.9 29 224.9 6.4 62 31 0.5 0.6 50 33 4.8 7.2 1376 34 2.5 2.3 121 64 6.3 2.3 6536.5 4.2 66 3.7 2.9 67 5.1 3.2 69 2.4 1.7 70 9 15.5 1490 71 0.8 1.3 22.472 124 32.6 1660 73 6.6 8.8 634 75 12.9 4.0 1212 76 1.5 1.3 43.4

The compounds of the present invention are particularly suitable for theinhibition of capsaicin induced hypothermie (table 3).

TABLE 3 Compound according Inhibition of capsaicin induced to examplehypothermie¹⁾ 2 73 3 55 10 49 12 36 13 7 19 71 20 31 21 32 31 88 34 8471 79 76 48 ¹⁾in comparison to vehicle control at maximum effect 15 minafter application of capsaicin; n = 5 (number of measurements)

The following table 4. includes the pharmacological data for examplecompounds 14 to 378.

IC₅₀ (human) inhibition K_(i) (rat) K_(i) (human) [nM] inhibitionhypothermie formaldehyde test (n = inhibition Bennet Example Cap. [nM]Cap. [nM] after pH stimulus (n = 5) 10) model (n = 10) 14 67.9 19.12386.0 15 12.0 3.5 148.0 16 0.8 0.2 14.7 0.3 po 12% 32 2.6 1.7 135.4 0.3po 55% 34 0.1 po 6% 0.3 po 51% 37 1.8 0.3 26.2 40 0.4 1.0 48 42 0.5 0.626 46 59.4 40% @ 5 μM 5% @ 1 μM 61 ne @ 1 μM ne @ 1 μM 47% @ 10 μM 62 ne@ 1 μM ne @ 1 μM ne @ 1 μM 63 23.9 28.6 70% @ 1 μM 71 0.3 po 0% 1 po 3%74 70% @ 10 μM 71% @ 10 μM 35% @ 10 μM 76 0.3 po 12% 77 57% @ 10 μM 21%@ 10 μM ne @ 1 μM 78 19% @ 1 μM 15% @ 1 μM 36% @ 10 μM 79 0.8 0.7 25.680 0.6 0.3 5.4 0.3 po 66% 0.3 po 58% 81 2.4 0.8 25.1 0.3 po 21% 82 0.70.9 16.2 0.3 po 53% 0.3 po 39% 1 po 43% 85 67.9 19.1 2386 87 143 36.12574 0.3 po 0% 88 5 0.3 57.1 0.3 po 38% 0.3 po 4% 1 po 16% 89 1.2 0.4130.8 0.3 po 1% 90 47 20.4 260 0.3 po 81% 0.3 po 46% 1 po 37% 91 0.5 0.529.9 0.1 po 30% 1 po 46% 10 po 43% 93 0.2 0.4 12.3 0.3 po 4% 94 0.3 po0% 95 0.8 0.5 52.6 96 0.5 30 97 44.5 2155 98 1.5 41 99 5.8 419 0.3 po 1%100 1.2 1.1 115.2 0.3 po 26% 101 1 0.3 40.5 102 7.4 4.2 18% @ 10 μM 1034.9 2.8 16 @ 10 μM 0.3 po 39% 0.3 po 36% 1 po 50% 104 0.2 0.2 40 0.0001po 20% 0.001 po 45% 0.01 po 49% 0.1 po 35% 106 0.5 0.5 18.6 0.1 po 24%0.3 po 21% 1 po 22% 10 po 84% 107 1 0.8 43.7 0.3 po 21% 108 0.6 1.4114.1 0.3 po 38% 0.3 po 15% 1 po 24% 109 0.6 0.7 30.7 110 63.1 59.6 13950.3 po 13% 111 3.5 0.9 90.1 112 31.8 39.2 64% @ 10 μM 26% @ 1 μM 112236.4 15% @ 1 μM 67% @ 25 μM 39% @ 10 μM 114 28.1 68.7 2357 115 10.915.8 203 116 6.6 9.1 293 0.3 po 21% 0.1 po 39% 0.3 po 57% 117 0.5 0.523.5 0.3 po 70% 0.3 po 5% 1 po 41% 118 0.2 0.2 7.6 120 0.4 0.7 51% @ 1μM 41% @ 0.1 μM 121 5.8 13.2 56% @ 10 μM 0.3 po 12% 32% @ 1 μM 122 0.60.7 40.4 0.3 po 33% 123 0.6 0.8 15.1 0.3 po 47% 124 0.4 0.3 5.1 0.3 po39% 125 1 0.9 23.8 0.1 po 5% 0.3 po 24% 0.01 po 17% 0.3 po 37% 1 po 19%0.1 po 30% 1 po 32% 1 po 46% 3 po 65% 3 po 40% 10 po 50% 126 1.2 o.9 1010.3 po 0% 0.1 po 20% 0.3 po 69% 127 0.6 0.5 15.4 0.3 po 6% 0.3 po 22% 1po 25% 128 1 0.7 27.8 129 1.6 1.8 77.2 0.3 po 10% 0.3 po 5% 1 po 3% 1304.5 2.1 34.3 0.3 po 58% 0.3 po 41% 1 po 55% 131 0.4 0.3 5.9 0.3 po 26%132 0.7 0.5 14.7 0.3 po 0% 133 0.7 2.1 62% @ 1 μM 38% @ 0.1 μM 134 335146 69% @ 25 μM 15% @ 1 μM 135 48.9 39.3 1160 136 8.3 14 140 0.3 po 43%0.01 po 13% 0.1 po 33% 1 po 47% 10 po 63% 137 1.9 0.7 12.5 0.3 po 9% 1381.2 0.5 19.8 0.3 po 0% 139 0.9 0.3 12.1 0.3 po 43% 140 0.4 0.7 9.2 0.1po 56% 0.3 po 73% 142 1.2 1 8.9 144 1 146 145 78 49% @ 10 μM 39% @ 5 μM2% @ 1 μM 147 1 0.7 10.4 0.3 po 3% 148 1.1 1.3 63.6 0.3 po 45% 0.3 po44% 1 po 46% 149 0.7 0.5 9.7 150 22.4 63.3 1320 0.3 po 17% 151 1.4 192.3 152 2.2 3.8 63% @ 10 μM 0.3 po 33% 45% @ 1 μM 1 po 24% 153 0.7 2.292.4 154 1.7 8.1 534 0.3 po 12% 155 0.8 1.8 145 156 1.7 1.4 69.8 157 1.32.9 43.1 158 12.6 4 139 159 21.4 2.4 280 0.3 po 28% 0.3 po 10% 1 po 14%160 3 3.5 28.2 0.3 po 28% 0.3 po 10% 1 po 14% 161 0.7 0.4 11.6 162 1.6 358% @ 1 μM 31% @ 0.1 μM 163 8.5 12.7 277 164 85%@10 μM; 84%@ 10 μM;28%@25 μM; 30%@10 μM 1.5%@1 μM 20%@1 μM 165 82%@ 25 μM; 76%@ 25 μM;40%@25 μM; 28%@10 μM 0.3 po 41% 0.3 po 29% 4%@ 10 μM 0.5%@ 10 μM 1 po15% 166 1.1 0.5 18.5 0.3 po 28% 0.3 po 48% 1 po 72% 167 2.8 0.8 21.3 0.3po 19% 0.1 po 62% 0.3 po 56% 168 1.4 0.9 17.6 0.3 po 21% 0.3 po 1% 1690.6 0.9 40.5 170 5.1 7.7 242 171 2.4 4.8 125 0.3 po 32% 0.3 po 45% 1 po46% 172 0.4 1.5 53 173 78.4 65.7 414 0.3 po 36% 0.3 po 0% 174 1.4 1.664.5 0.3 po 39% 0.3 po 5% 1 po 49% 175 1.2 2.5 25 176 60%@10 μM8% 63%@10 μM 43%@10 μM. 13%@1 μM @1 μM 7.2%@ 1 μM 177 34%@1 μM 51 1290 0.3 po14% 0.3 po 31% 9%@0.1 μM 1 po 24% 178 1.9 0.5 27.6 0.3 po 42% 0.3 po 16%1 po 28% 179 1 1.1 23.1 0.3 po 57% 0.3 po 5% 1 po 22% 180 0.3 0.8 22.8181 5.6 14.6 1074 182 7.3 4.2 637 0.3 po 45% 0.3 po 1% 1 po 8% 183 0.70.6 10.5 184 77 59 ne @ 1 μM 185 49.1 425 ne @ 1 μM 186 0.8 0.6 37.6 1870.5 1 39.6 188 5 5 192 0.3 po 0% 189 3 4.7 166 190 0.4 0.6 31 191 2 2.285 192 2.4 1.4 47 193 3.2 2.1 69%@1 μM 58%@0.1 μM8%@0.01 μM 194 3.8 4.121% @ 1 μM 0.3 po 14% 0% @ 0.1 μM 195 0.4 1.1 61 196 0.4 0.6 41%@1 μM48%@0.1 μM6%@0.01 μM 197 0.4 1.5 97.3 198 0.9 6.4 31%@1 μM 11%@0.1 μM199 1.6 1.4 31 200 3.4 4.2 81 201 1.2 2.4 34 202 24.8 29.5 30%@1 μM16%@0.1 μM 203 3.3 3 24%@1 μM 0%@0.1 μM 204 1.6 4 148.1 205 11.4 0.957.4 206 0.7 3.2 66.1 207 0.8 0.8 38.6 208 0.5 0.6 38.6 209 0.2 0.9 34.93 po 46% 210 0.2 0.3 8 211 30.3 142 3441 212 3.6 4.2 33%@1 μM 11%@0.1 μM213 2.0 2.8 49%@10 μM 37%@1 μM 214 1.5 1.4 108.2 215 48% @10 μM 37% @10μM 15%@25 μM 4%@1 μM 216 0.5 2.0 64.7 0.3 po 4% 217 1.1 2.8 36.5 0.1 po40% 0.3 po 9% 0.3 po 97% 1 po 37% 218 0.4 1.3 13.8 219 2.4 3.3 38.3 2202.4 3.4 39.2 221 1.9 2.5 44.5 0.3 po 18% 222 2.4 3.4 39.2 223 53%@1 μM38%@1 μM ne @ 1 μM 4%@0.1 μM 225 0.5 0.7 27.3 0.3 po 20% 226 1.5 2 45.2227 348 91 51%@10 μM 7%@1 μM 228 2.5 1.3 612 229 0.7 0.7 17.7 230 0.60.4 20.1 231 0.8 1.4 37.6 233 1.4 2.5 63%@ 10 μM 50%@1μ 234 1.0 1.5 85.30.1 po 19% 0.03 po 5% 0.001 po 26% 0.3 po 31% 0.1 po 28% 0.01 po 48% 0.3po 41% 0.1 po 53% 1 po 44% 1 po 65% 235 0.6 0.9 55 236 1.4 2.7 69%@ 10μM 76%@1 μM 2%@0.1 μM 237 2.0 4.4 70%@ 1 μM 238 0.6 0.7 55%@ 1 μM; 39%@0.1 μM 3%@ 0.01 μM 240 5.3 1.2 43%@ 1 μM 12%@0.1 μM 241 0.5 1.9 79%@1 μM34%@0.1 μM 242 1.2 3.7 165 243 5.1 16 337 244 1.1 2.1 182 245 1.7 2.774%@1 μM 21%@0.1 μM 246 0.5 0.7 87 247 0.5 1.8 69%@1 μM 36%@0.1 μM 2480.9 3.9 74%@25 μM 66%@10 μM 63%@1 μM 249 0.2 1.6 70%@1 μM 31%@0.1 μM 2500.9 0.9 68%@ 10 μM 51% @ 1 μM 24% @ 0.1 μM 251 8.7 3.8 281 252 17.9 6.1289 254 1.3 4.2 63% @ 1 μM 19%@0.1 μM 255 1.3 0.9 101 256 0.3 0.6 (1.5)59%@1 μM 43%@0.1 μM15%@0.01 μM 257 0.3 0.6 67%@1 μM 63%@0.1 μM11%@0.01μM 258 1.3 2.5 132 259 22.8 15.4 47%@10 μM 51%@1 μM 0%@0.1 μM 260 25.321.6 66%@10 μM 51%@1 μM 8.5%@ 0.1 μM 261 ne @ 1 μM 262 1.7 1.2 58%@1 μM6%@0.1 μM 263 0.7 0.6 63%@1 μM 52%@0.1 μM4%@0.01 μM 264 0.9 0.6 15.9 2652.5 5 33% @ 1 μM 17%@0.1 μM 266 3.4 ne @ 1 μM 267 1.7 1.6 24 268 0.8 0.917 269 ne @ 1 μM ne @ 1 μM ne @ 1 μM 270 0.5 0.7 19.7 271 1.1 1.0 44.4273 11.5 1605 274 0.7 63 275 20.3 1189 276 78%@ 5 μM 43%@5 μM 11%@1 μM11%@ 35%@1 μM 0.1 μM 14%@ 0.1 μM 278 0.4 76 279 1.7 1.1 161 282 1.2 0.862%@10 μM 57%@1 μM 55%@0.1 μM12%@0.01 μM 283 4.5 2.9 51%@10 μM 51%@1 μM43%@0.1 μM11%@0.01 μM 284 48 54.9 ne @ 1 μM 285 4.5 3.5 377 287 3.5 4.4189 288 41 42 ne @ 1 μM 289 3.3 2.5 ne @ 1 μM 290 4.4 480 0.1 po 24% 0.3po 78% 1 po 68% 291 0.6 43.4 292 32.7 63%@ 5 μM; 6% @ 1 μM 293 1.4 129294 1.9 304 295 0.6 25 296 0.9 154 297 2.5 179 298 1.6 183 299 1 43 3002.1 59.5 301 0.9 102 302 100.1 1182 303 1.8 76.2 304 0.71 35.4 307 5.0456 308 3.2 414.5 309 8.7 20% bei 5 μM 310 43.7 27% bei 5 μM 311 1.431092.0 312 68% @ 5 μM ne @ 1 μM 7% @ 1 μM 313 2.7 ne @ 1 μM 314 46% @ 5μM 31%@10 μM 14%@5 μM 12% @ 1 μM 315 1 295 316 72.1 ne @ 1 μM 317 1.7 43318 17.5 32%@10 μM 4%@5 μM 319 13.8 54%@10 μM 38%@5 μM 4%@1 μM 320 1.136 321 0.8 38 322 1 54% @ 1 μM 25% @ 0.1 μM 323 1.9 41% @ 1 μM 15% @ 0.1μM 324 0.6 33 325 8.6 716 326 25.6 66% @ 10 μM 32% @ 5 μM 8% @ 1 μM 3273.4 342 328 0.8 128 329 0.8 179 1 po 7% 1 po 54% 330 31.3 806 1 po 7% 1po 54% 1 iv 7% 331 0.7 31% @ 10 μM 22% @ 5 μM 26% @ 1 μM 18% @ 0.1 μM332 2.4 159 334 0.7 99 335 1.1 ne @ 1 μM 336 0.7 50%@ 1 μM 35%@ 0.1 μM28%@ 0.05 μM 337 0.7 30% @ 10 μM 6% @ 5 μM 338 0.9 140 339 0.3 14 3401.2 279 341 1.3 293 342 19.3 1139 343 55% @ 5 μM ne @ 1 μM 8% @ 1 μM 34434% @ 5 μM ne @ 1 μM 3% @ 1 μM 345 2.8 45% @ 5 μM 38% @ 1 μM 3% @ 0.1 μM346 0.7 66 347 1.6 349 44 ne @ 1 μM 350 5.8 52% @ 1 μM 4% @ 0.1 μM 35144 ne @ 1 μM 352 0.5 61% @ 10 μM 34% @ 5 μM 27% @ 1 μM 353 0.6 25% @ 1μM 28% @ 0.1 μM 18% @ 0.05 μM 354 0.8 85 355 15.3 2205 356 9.2 ne @ 1 μM361 9.7 462 362 1.5 161 363 0.7 76 369 1.7 182 370 5.6 250 371 3.7 368372 14.3 52% @ 1 μM 373 14.8 492 374 2.3 314 375 0.7 30 376 0.8 20 377 3378 23.9 325 The dosis is in each case given in mg/kg body weight;wherein po describes peroral administration and iv intravenousadministration. ne denotes in each case “no effect”, d.h. no reactionwas observed. The value given after the symbol “@” denotes theconcentration at which the inhibition (given in percent) was determinedin each case.

1. Substituted compounds of the general formula A,

in which X denotes O, S or N—CN; Y denotes —NH₂; —NHR³⁰; —NR³¹R³² or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; n denotes 0, 1, 2, 3 or 4; R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³, —S(═O)₂—R²⁴; —S(═O)—R²⁴; denotes a linear or branched, unsaturated or saturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue, optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue; T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R¹⁰; R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I; —SF_(S); —NO₂; —CF₃; —CF₂C1; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³, —S(═O)—R²⁴; —S(═O)₂—R²⁴; or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denote an unsubstituted or at least monosubstituted 6- or 10-membered aryl residue, which may be attached via a linear or branched, substituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; R¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂C1; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NH R²⁸)(NHR²⁹); denotes a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀ residue, which is in each case substituted with optionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅ alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃; denotes an unsubstituted C₂₋₁₀ alkenyle residue or an unsubstituted C₂₋₁₀ alkynyle residue; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group; R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³, R²⁴, R²⁷, R²⁸ and R²⁹, mutually independently, in each case denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; denote an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to 6-membered heteroalkylene group; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to 6-membered heteroalkylene group; or R¹² and R¹³, in each case together with the nitrogen atom joining them together as a ring member, form a saturated or unsaturated, unsubstituted or at least monosubstituted 4-, 5-, 6-, 7-, 8- or 9-membered heterocycloaliphatic residue optionally comprising at least one further heteroatom as ring member, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system; and R²⁵ and R²⁶, mutually independently, in each case denote a hydrogen residue; denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denote an unsaturated or saturated, unsubstituted or at least monosubstituted, 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member; providing that R²⁵ and R²⁶ do not in each case denote a hydrogen residue; or R²⁵ and R²⁶, together with the carbon atom joining them together as a ring member, form a saturated or unsaturated, unsubstituted or at least monosubstituted 3-, 4-, 5- or 6-membered cycloaliphatic residue; and R³⁰, R³¹ and R³², mutually independently, in each case denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 2. Substituted compounds of general formula I according to claim 1,

in which X denotes O, S or N—CN; n denotes 0, 1, 2, 3 or 4; R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³, —S(═O)₂—R²⁴; —S(═O)—R²⁴; denotes a linear or branched, unsaturated or saturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue, optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue; T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R¹⁰; R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁸; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³, —S(═O)—R²⁴; —S(═O)₂—R²⁴; or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denote an unsubstituted or at least monosubstituted 6- or 1 0-membered aryl residue, which may be attached via a linear or branched, substituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; R⁸ denotes H; F; Cl; Br; I; —SF_(S); —NO₂; —CF₃; —CF₂C1; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁸; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; R¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂C1; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀ residue, which is in each case substituted with optionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅ alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃; denotes an unsubstituted C₂₋₁₀ alkenyle residue or an unsubstituted O₂₋₁₀ alkynyle residue; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group; R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³, R²⁴, R²⁷, R²⁸ and R²⁹, mutually independently, in each case denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; denote an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to 6-membered heteroalkylene group; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to 6-membered heteroalkylene group; or R¹² and R¹³, in each case together with the nitrogen atom joining them together as a ring member, form a saturated or unsaturated, unsubstituted or at least monosubstituted 4-, 5-, 6-, 7-, 8- or 9-membered heterocycloaliphatic residue, optionally comprising at least one further heteroatom as ring member, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system; and R²⁵ and R²⁶, mutually independently, in each case denote a hydrogen residue; denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denote an unsaturated or saturated, unsubstituted or at least monosubstituted, 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member; providing that R²⁵ and R²⁶ do not in each case denote a hydrogen residue; or R²⁵ and R²⁶, together with the carbon atom joining them together as a ring member, form a saturated or unsaturated, unsubstituted or at least monosubstituted 3-, 4-, 5- or 6-membered cycloaliphatic residue; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 3. Compounds according to claim 1, characterized in that in which X denotes O, S or N—C≡N; n denotes 0, 1, 2, 3 or 4; R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³, —S(═O)₂—R²⁴; —S(═O)—R²⁴; denotes a linear or branched, unsaturated or saturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue, optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue; T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R¹⁰; R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³, —S(═O)—R²⁴; —S(═O)₂—R²⁴; or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denote an unsubstituted or at least monosubstituted 6- or 10-membered aryl residue, which may be attached via a linear or branched, substituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; R¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NH R²⁸)(NH R²⁹); denotes a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀ residue, which is in each case substituted with optionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅ alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃; denotes an unsubstituted C₂₋₁₀ alkenyle residue or an unsubstituted C₂₋₁₀ alkynyle residue; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group; R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³, R²⁴, R²⁷, R²⁸ and R²⁹, mutually independently, in each case denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; denote an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to 6-membered heteroalkylene group; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to 6-membered heteroalkylene group; or R¹² and R¹³, in each case together with the nitrogen atom joining them together as a ring member, form a saturated or unsaturated, unsubstituted or at least monosubstituted 4-, 5-, 6-, 7-, 8- or 9-membered heterocycloaliphatic residue, optionally comprising at least one further heteroatom as ring member, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system; and R²⁵ and R²⁶, mutually independently, in each case denote a hydrogen residue; denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denote an unsaturated or saturated, unsubstituted or at least monosubstituted, 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member; providing that R²⁵ and R²⁶ do not in each case denote a hydrogen residue; or R²⁵ and R²⁶, together with the carbon atom joining them together as a ring member, form a saturated or unsaturated, unsubstituted or at least monosubstituted 3-, 4-, 5- or 6-membered cycloaliphatic residue; wherein unless otherwise stated, the above-stated aliphatic C₁₋₁₀ residues may optionally in each case be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅-alkyl), —S(C₁₋₅-alkyl), —NH(C₁₋₅-alkyl), —N(C₁₋₅-alkyl)(C₁₋₅-alkyl), —O(═O)—O—C₁₋₅-alkyl, —O—C(═O)—C₁₋₅-alkyl, —O-phenyl, phenyl, —OCF₃ and —SCF₃; the above-stated 2- to 6-membered heteroalkylene groups, C₁₋₆-alkylene groups, C₂₋₆-alkenylene groups and C₂₋₆-alkynylene groups may optionally in each case be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅-alkyl), —S(C₁₋₅-alkyl), —NH(C₁₋₅-alkyl), —N(C₁₋₅-alkyl)(C₁₋₅-alkyl), —OCF₃ and —SCF₃; the above-stated heteroalkylene groups may in each case optionally comprise 1, 2 or 3 heteroatom(s) mutually independently selected from the group consisting of oxygen, nitrogen (NH) and sulfur; the above-stated (hetero)cycloaliphatic residues may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C₁₋₆-alkylene-OH, ═CH₂, —O—C₁₋₅-alkylene-oxetanyl, —C₁₋₅-alkylene-O—C₁₋₅-alkylene-oxetanyl, —CH₂—NH—C₁₋₅-alkyl, —CH₂—N(C₁₋₅-alkyl)₂, —N[C(═O)—C₁₋₅-alkyl]-phenyl, —CH₂—O—C₁₋₅-alkyl, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —O—C(═O)—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—C₁₋₅-alkyl, —C(═O)—OH, —O(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —NH-phenyl, —N(C₁₋₅-alkyl)-phenyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N[C(═O)—C₁₋₅-alkyl]-phenyl, —NH-phenyl, —N(C₁₋₅-alkyl)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; and the above-stated (hetero)cycloaliphatic residues may in each case optionally comprise 1, 2 or 3 (further) heteroatom(s) mutually independently selected from the group consisting of oxygen, nitrogen and sulfur; the rings of the above-stated mono- or polycyclic ring systems may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—C₁₋₅-alkyl, —O(═O)—OH, —O(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl, and the rings of the above-stated mono- or polycyclic ring systems are in each case 5-, 6- or 7-membered and may in each case optionally comprise 1, 2, 3, 4 or 5 heteroatom(s) as ring member(s), which are mutually independently selected from the group consisting of oxygen, nitrogen and sulfur; and the above-stated aryl or heteroaryl residues may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—OH, —O(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —NH—S(═O)₂—C₁₋₅-alkyl, —NH—C(═O)—O—C₁₋₅-alkyl, —C(═O)—H, —O(═O)—C₁₋₅-alkyl, —C(═O)—NH₂, —O(═O)—NH—C₁₋₅-alkyl, —C(═O)—N—(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl, and the above-stated heteroaryl residues in each case optionally comprise 1, 2, 3, 4 or 5 heteroatom(s) mutually independently selected from the group consisting of oxygen, nitrogen and sulfur as ring member(s); in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 4. Compounds according to claim 1, characterized in that n, X, Y, T, U, V, W, R¹ to R⁷, R⁹ and R¹¹ to R³² have the meaning as defined in claim 1 and R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a saturated or unsaturated, unsubstituted or at least monosubstituted chain comprising 1 to 7 carbon atoms as chain members, wherein 1, 2 or 3 carbon atoms can be replaced by heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen (NH); denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; and R¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂C1; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —C(═O)—NHR¹⁸; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a saturated or unsaturated, unsubstituted or at least monosubstituted chain comprising 1 to 7 carbon atoms as chain members, wherein 1, 2 or 3 carbon atoms can be replaced by heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen (NH), which, in the absence of any heteroatoms as chain members, is substituted with optionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅ alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group.
 5. Compounds according to claim 4, characterized in that n, X, Y, T, U, V, W, R¹ to R⁷, R⁹ and R¹¹ to R³² have the meaning as defined in claim 4 and R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a saturated or unsaturated, unsubstituted or at least monosubstituted chain comprising 5 to 7 carbon atoms as chain members, wherein 1, 2 or 3 carbon atoms can be replaced by heteroatoms selected from the group consisting of oxygen and sulfur; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; and R¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —C(═O)—NHR¹⁸; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a saturated or unsaturated, unsubstituted or at least monosubstituted chain comprising 5 to 7 carbon atoms as chain members, wherein 1, 2 or 3 carbon atoms can be replaced by heteroatoms selected from the group consisting of oxygen and sulfur, which, in the absence of any heteroatoms as chain members, is substituted with optionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅ alkyl), —S(C₁₋₅ alkyl), —NH(C₁₋₅ alkyl), —N(C₁₋₅ alkyl)(C₁₋₅ alkyl), —OCF₃ and —SCF₃; denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group; or denotes an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group.
 6. Compounds of general formula B1 according to claim 1,

in which X denotes O, S or N—C≡N; n denotes 0, 1, 2, 3 or 4; R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C═O—R²³, —S(═O)₂—R²⁴; —S(═O)—R²⁴; denotes a linear or branched, unsaturated or saturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denotes an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue, optionally comprising at least one heteroatom as a ring member, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue; T denotes C—R⁶ and U denotes C—R⁷ and V denotes N; or T denotes C—R⁶ and U denotes N and V denotes C—R⁹; or T denotes N and U denotes C—R⁷ and V denotes C—R⁹; or T denotes N and U denotes N and V denotes C—R⁹; or T denotes N and U denotes C—R⁷ and V denotes N; or T denotes C—R⁶ and U denotes N and V denotes N; R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³, —S(═O)—R²⁴; —S(═O)₂—R²⁴; or denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; or denote an unsubstituted or at least monosubstituted 6- or 10-membered aryl residue, which may be attached via a linear or branched substituted or at least monosubstituted C₁₋₆ alkylene croup or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes a linear or branched saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³, and R²⁴, mutually independently, in each case denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residue; denote an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member, which residue may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or 2- to 6-membered heteroalkylene group; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched unsubstituted or at least monosubstituted C₁₋₆ alkylene croup or 2- to 6-membered heteroalkylene group; or R¹² and R¹³, in each case together with the nitrogen atom joining them together as a ring member, form a saturated or unsaturated, unsubstituted or at least monosubstituted 4-, 5-, 6-, 7-, 8- or 9-membered heterocycloaliphatic residue, optionally comprising at least one further heteroatom as ring member, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system; R²⁵ and R²⁶, mutually independently, in each case denote a hydrogen residue; denote a linear or branched, saturated or unsaturated, unsubstituted or at least monosubstituted aliphatic C₁₋₁₀ residuez or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denote an unsaturated or saturated, unsubstituted or at least monosubstituted, 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue optionally comprising at least one heteroatom as a ring member; providing that R²⁵ and R²⁶ do not in each case denote a hydrogen residue: or R²⁵ and R²⁶, together with the carbon atom joining them together as a ring member, form a saturated or unsaturated, unsubstituted or at least monosubstituted 3-, 4-, 5- or 6-membered cycloaliphatic residue; wherein unless otherwise stated the above-stated aliphatic C₁₋₁₀ residues may optionally in each case be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅-alkyl), —S(C₁₋₅-alkyl), —NH(C₁₋₅-alkyl), —N(C₁₋₅-alkyl)(C₁₋₅-alkyl), —C(═O)—O—C₁₋₅-alkyl, —O—C(═O)—C₁₋₅-alkyl, —O-phenyl, phenyl, —OCF₃ and —SCF₃; the above-stated 2- to 6-membered heteroalkylene group, C₁₋₆-alkylene groups, C₂₋₆-alkenylene groups and C₂₋₆-alkynylene groups may optionally in each case be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O(C₁₋₅-alkyl), —S(C₁₋₅-alkyl), —NH(C₁₋₅-alkyl), —N(C₁₋₅-alkyl)(C₁₋₅alkyl), —OCF₃ and —SCF₃; the above-stated heteroalkylene groups may in each case optionally comprise 1, 2 or 3 heteroatom(s) mutually independently selected from the group consisting of oxygen, nitrogen (NH) and sulfur; the above-stated (hetero)cycloaliphatic residues may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C₁₋₆-alkylene-OH, ═CH₂—O—C₁₋₅-alkylene-oxetanyl, —C₁₋₅-alkylene-O—C₁₋₅-alkylene-oxetanyl, —CH₂—NH—C₁₋₅-alkyl, —CH₂—N(C₁₋₅-alkyl)₂, —N[C(═O)—C₁₋₅-alkyl]-phenyl, —CH₂—O—C₁₋₅-alkyl, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃—SF₅, —OH, —O—C₁₋₅-alkyl, —O—C(═O)—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—C₁₋₅-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅-alkyl, —NH-phenyl, —N(C₁₋₅-alkyl)-phenyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazol, thiazol, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazol, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N[C(═O)—C₁₋₅-alkyl]-phenyl, —NH-phenyl, —N(C₁₋₅-alkyl)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; and the above-stated (hetero)cycloaliphatic residues may in each case optionally comprise 1, 2 or 3 (further) heteroatom(s) mutually independently selected from the group consisting of oxygen, nitrogen and sulfur; the rings of the above-stated mono- or polycyclic ring systems may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃—SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂—NO₂—O—CF₃—S—CF₃—SH, —S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—C₁₋₅-alkyl, —C(═O)—OH—C(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl, and the rings of the above-stated mono- or polycyclic ring systems are in each case 5-, 6- or 7-membered and may in each case optionally comprise 1, 2, 3, 4 or 5 heteroatom(s) as ring member(s), which are mutually independently selected from the group consisting of oxygen, nitrogen and sulfur; and the above-stated aryl or heteroaryl residues may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —CF₃—SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂—NO₂, —O—CF₃—S—CF₃, —SH, —S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—OH, —O(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —NH—S(═O)₂—C₁₋₅-alkyl, —NH—C(═O)—O—C₁₋₅-alk-C(═O)—H—C(═O)—C₁₋₅-alkyl, —C(═O)—NH₂—C(═O)—NH—C₁₋₅-alkyl, —C(═O)—N—(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃—, SF₅, —CN, —NO₂—, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃—S—CF₃, phenyl and —O-benzyl, and the above-stated heteroaryl residues in each case optionally comprise 1, 2, 3, 4 or 5 heteroatom(s) mutually independently selected from the group consisting of oxygen, nitrogen and sulfur as ring member(s); D denotes CH or N; p denotes 0, 1, 2 or 3; q denotes 0, 1, 2 or 3; K, L and M, mutually independently, in each case denote H, F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —C(═O)—OH, —C(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —NH—S(═O)₂—C₁₋₅-alkyl, —NH—C(═O)—O—C₁₋₅-alkyl, —C(═O)—H, —C(═O)—C₁₋₅-alkyl, —C(═O)—NH₂, —C(═O)—NH—C₁₋₅-alkyl, —C(═O)—N—(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF_(S), —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; W denotes —CN, —NR³⁴R³⁵, —C(═O)—R³⁶ or —C(═O)—OR³⁷; and R³⁴, R³⁵, R³⁶ and R³⁷, mutually independently, in each case denote hydrogen or denote a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀ residue denote an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆-alkenylene group or C₂₋₆-alkynylene group.
 7. Compounds of general formula B2 according to claim 6,

in which U, T, V, X, n, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have the meaning as defined in claim 6; D denotes CH or N; q denotes 0, 1, 2 or 3; K, L and M, mutually independently, in each case denote H, F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—C₁₋₅-alkyl, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—C₁₋₅-alkyl, —C₁₋₅-alkyl, —O(═O)—OH, —O(═O)—O—C₁₋₅-alkyl, —NH—C₁₋₅-alkyl, —N(C₁₋₅-alkyl)₂, —NH—S(═O)₂—C₁₋₅-alkyl, —NH—C(═O)—O—C₁₋₅-alkyl, —C(═O)—H, —O(═O)—C₁₋₅-alkyl, —C(═O)—NH₂, —O(═O)—NH—C₁₋₅-alkyl, —O(═O)—N—(C₁₋₅-alkyl)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; and R³⁴ and R³⁵, mutually independently, in each case denote hydrogen or denote a linear or branched, saturated or unsaturated aliphatic C₁₋₁₀ residue; denote an unsaturated or saturated, unsubstituted or at least monosubstituted 3-, 4-, 5-, 6-, 7-, 8- or 9-membered cycloaliphatic residue, which residue is in each case attached to the parent structure via a carbon atom in the ring of the cycloaliphatic residue and may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆ alkenylene group or C₂₋₆ alkynylene group; or denote an unsubstituted or at least monosubstituted 5- to 14-membered aryl or heteroaryl residue, which may be fused with a saturated or unsaturated, unsubstituted or at least monosubstituted mono- or polycyclic ring system and/or be attached via a linear or branched, unsubstituted or at least monosubstituted C₁₋₆ alkylene group or C₂₋₆-alkenylene group or C₂₋₆-alkynylene group.
 8. Compounds according to claim 1, characterized in that X denotes O, S or N—CN; n denotes 0, 1, 2, 3 or 4; R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CN; —CF₃; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote an alkyl residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl and n-heptyl; R⁵ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; denotes an alkyl residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl and n-heptyl; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R¹⁰; R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²⁰R²¹; —C(═O)—OR²²; —C(═O)—R²³, —S(═O)—R²⁴; —S(═O)₂—R²⁴; denote an alkyl residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl and n-heptyl or denote a phenyl residue, which may be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁶; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴, —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes an alkyl residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-yl, n-hexyl and n-heptyl; denotes an alkenyl residue selected from the group consisting of 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, (3,3)-dimethyl-but-1-enyl, ethenyl, propenyl, butenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and 1-pentenyl; denotes an alkynyl residue selected from the group consisting of ethynyl, propynyl, butynyl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl and pentynyl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and tthiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —CEO— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)— phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; or denotes a residue selected from the group consisting of tetrazolyl, phenyl, naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]thiophenyl, benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyl and isochinolinyl, wherein the residue may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁸; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes an alkyl residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl and n-heptyl; R¹⁰ denotes —SF₅; —NO₂; —CF₃; —CF₂Cl; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—NHR¹⁸; —C(═O)—NR¹⁷R¹⁸; —S(═O)₂—NHR¹⁹; —S(═O)₂—NR²OR²¹; —C(═O)—OR²²; —C(═O)—R²³; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes an alkyl residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl and n-heptyl which is in each case substituted with optionally 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —OCF₃ and —SCF₃; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, cycloheptenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and tthiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)— phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF_(S), —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; or denotes a residue selected from the group consisting of tetrazolyl, phenyl, naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]thiophenyl, benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyl and isochinolinyl, wherein the residue may in each case be attached via a —(CH═CH)—, —C≡O—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —O(═O)—OH, —O(═O)—O—CH₃, —O(═O)—O—O₂H₅, —O(═O)—O—CH(CH₃)₂, —O(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—O₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—O₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NH—C(═O)—O—O₂H₅, —NH—C(═O)—O—C(CH₃)₃, —O(═O)—H, —C(═O)—OH₃, —O(═O)—O₂H₅, —O(═O)—CH(OH₃)₂, —O(═O)—O(OH₃)₃, —O(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —O(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R¹⁶, R¹⁷, R¹⁸, R¹⁹, R²⁰, R²¹, R²², R²³, R²⁴, R²⁷, R²⁸ and R²⁹, mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl, n-heptyl, 3-pentyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclopentenyl, cyclohexenyl, Cycloheptenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, wherein the residue may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; or denote a residue selected from the group consisting of phenyl, naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl, benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyl and isochinolinyl, wherein the residue may in each case be attached via a —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —O(═O)—OH, —O(═O)—O—CH₃, —O(═O)—O—O₂H₅, —O(═O)—O—CH(CH₃)₂, —O(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(O₂H₅), —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —O(═O)—H, —C(═O)—CH₃, —O(═O)—O₂H₅, —C(═O)—CH(CH₃)₂, —O(═O)—C(CH₃)₃, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—O₂H₅, —C(═O)—N(CH₃)₂, —O(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, —C₁₋₅-alkyl, —O—C₁₋₅-alkyl, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; or R¹² and R¹³ in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,3,4,5)-tetrahydropyrido[4,3-b]indolyl, (3,4)-dihydro-1H-isochinolinyl, (1,3,4,9)-tetrahydro-[b]-carbolinyl, imidazolidinyl, (1,3)-thiazolidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CH₂—O—OH₂-oxetanyl, —CH₂—OH, —CH₂—OH₂—OH, ═CH₂, —O—CH₂-oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, piperidinyl, pyrrolidinyl, cyclohexyl, cyclopentyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; and R²⁵ and R²⁶, mutually independently, in each case denote a hydrogen residue; denote an alkyl residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl, isobutyl, n-pentyl, n-hexyl and n-heptyl; denote a residue selected from the group consisting of phenyl, naphthyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, benzo[b]furanyl, benzo[b]thiophenyl, benzoxazolyl, benzisoxazolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyl and isochinolinyl, wherein the residue may in each case be attached via a —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyln-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denote a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl; providing that R²⁵ and R²⁶ do not in each case denote a hydrogen residue; or R²⁵ and R²⁶ in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl; wherein unless otherwise stated, the above-stated alkyl, alkenyl and alkynyl residues may in each case optionally be substituted with 1, 2, 3, 4, 5, 6, 7, 8 or 9 substituents mutually independently selected from the group consisting of alkenyl-C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—C(CH₃)₃, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—CH(CH₃)₂, —O—C(═O)—C(CH₃)₃, —O-phenyl, phenyl, F, Cl, Br, I, —CN, —NO₂, —OH, —NH₂, —SH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —OCF₃ and —SCF₃; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 9. Compounds according to claim 1, characterized in that X denotes O, S or N—CN; Y denotes —NH₂; —NHR³⁰; —NR³¹R³²; denotes an alkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl; n denotes 0, 1, 2, 3 or 4; R¹, R², R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br; I; —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denote a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, n-butyln-butyl, sec-butyl, isobutyl and tert-butyl; R⁵ denotes F; Cl; Br; I; —SF₅; —OR¹⁴; —SR¹⁵; —S(═O)—R²⁴; —S(═O)₂—R²⁴; denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CH₂—CN, —CH₂—O—CH₃, —CH₂—O—CF₃, —CH₂—CF₃, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, —CH₂—CH₂—CN, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, —CH₂—CH₂—CH₂—CN, —CH₂—O—CH₂—CH₃, —CH₂—CH₂—SF₃, —CH₂—CH₂—OCF₃, —CH(CH₃)(O—CH₃), —CH(CH₃)(S—CH₃), n-butyl, —CF₂—CF₂—CF₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CN, n-butyl, sec-butyl, isobutyl, —C(CH₃)₂(CH₂OH), and tert-butyl; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl, which may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of oxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R¹⁰; R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I; —SF_(S); —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—OR²²; —S(═O)—R²⁴; —S(═O)₂—R²⁴; denote a residue selected from the group consisting of —CH₂—OH, methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl or denote a phenyl residue, which may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; R⁸ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—OR²²; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, sec-pentyl, neo-pentyl, n-hexyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, (3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-enyl, ethenyl, propenyl, butenyl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, ethynyl, propynyl, butynyl, pentynyl, —CF═CF₂, —CCl═Cl₂, —CH₂—CF═CF₂, —CH₂—CCl═CCl₂, —C≡C—I, —C≡C—F and —C≡C—Cl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CN, —CH₂—N(CH₃)₂₃—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denotes a residue selected from the group consisting of (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, tetrazolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyl and isochinolinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂₃—C(═O)—C(CH₃)₃₃—C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl; R⁹ denotes H; F; Cl; Br; I; —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —S(═O)—R²⁴; —S(═O)₂—R²⁴ or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂OI, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R¹⁰ denotes —SF₅; —NO₂; —CN; —NH₂; —OH; —SH; —C(═O)—NH₂; —S(═O)₂—NH₂; —C(═O)—NH—OH; —C(═O)—OH; —C(═O)—H; —S(═O)₂—OH; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—OR²²; —S(═O)—R²⁴; —S(═O)₂—R²⁴; —C(═NH)—NH₂; —C(═NH)—NH—R²⁷; —N═C(NH₂)₂; —N═C(NHR²⁸)(NHR²⁹); denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CN, —CH₂—N(CH₃)₂₃—CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denotes a residue selected from the group consisting of (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, tetrazolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyl and isochinolinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —ON, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(OH₃)(O₂H₅), —NH—C(═O)—O—CH₃, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NH—C(═O)—O—O₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H, —C(═O)—CH₃, —O(═O)—C₂H₅, —O(═O)—CH(CH₃)₂, —O(═O)—C(OH₃)₃, —O(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl; R¹¹, R¹², R¹³, R¹⁴, R¹⁵, R²², R²⁴, R²⁷, R²⁸ and R²⁹, mutually independently, in each case denote a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CH₂—ON, —CH₂—O—CH₃, —CH₂—O—CF₃, —CH₂—CF₃, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, —CH₂—CH₂—ON, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, —CH₂—CH₂—CH₂—ON, —CH₂—O—CH₂—CH₃, —CH₂—CH₂—SF₃, —CH₂—CH₂—OCF₃, —CH(CH₃)(CH₃)₃—CH(CH₃)(S—CH₃), n-butyl, —CF₂—CF₂—CF₂—CF₃, —CH₂—CH₂—CH₂—CH₂—ON, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, imidazolidinyl, tetrahydrofuranyl, tetrahydrothiophenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting ofoxo (═O), thioxo (═S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —O(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, thiazolyl, oxazolyl and isoxazolyl, which may in each case be attached via a —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH—C(═O)—O—CH₃, —NH—C(═O)—O—C₂H₅, —NH—C(═O)—O—C(CH₃)₃, —C(═O)—H, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—NH₂, —C(═O)—NH—CH₃, —C(═O)—NH—C₂H₅, —C(═O)—N(CH₃)₂, —C(═O)—N(C₂H₅)₂, —O-phenyl, —O-benzyl, phenyl and benzyl; or R¹² and R¹³ in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —O—CH₂-oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)— pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl, and R²⁵ and R²⁶, mutually independently, in each case denote a hydrogen residue; denote an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl; denote a residue selected from the group consisting of phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl, pyrazolyl, pyrazinyl, pyranyl, triazolyl, pyridinyl, imidazolyl, indolyl, isoindolyl, thiazolyl, oxazolyl, isoxazolyl, pyridazinyl, pyrazinyl, pyrimidinyl, indazolyl, chinoxalinyl, chinolinyl and isochinolinyl, which may in each case be attached via a —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denote a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; providing that R²⁵ and R²⁶ do not in each case denote a hydrogen residue; or R²⁵ and R²⁶ in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; and R³⁰, R³¹ and R³², mutually independently, in each case denote an alkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 10. Compounds according to claim 1, characterized in that X denotes O, S or N—CN; Y denotes —NH₂; —NHR³⁰; —NR³¹R³²; denotes an alkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl; n denotes 0, 1 or 2; R¹, R³ and R⁴, mutually independently, in each case denote H; F; Cl; Br; or denote a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂C1 and —CFCl—CF₂O₁; R² denotes F; Cl; Br; I or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—C₂H₅, —O—CF₂—CH₃, —O—CH₂—CF₃, —O—C₂F₅, —O—CH₂—CCl₃, —O—CH₂—CBr₃, —O—CHF—CF₂Cl, —O—CF₂—CF₂Cl, —O—CFCl—CF₂Cl, —O—CH₂—CH₂—CH₃, —O—CF₂—CF₂—CF₃, —O—CF(CF₃)₂, —O—CH(CH₃)₂, —O—C(CH₃)₃, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—C₂H₅, —S—CF₂—CH₃, —S—CH₂—CF₃, —S—C₂F₅, —S—CH₂—CCl₃, —S—CH₂—CBr₃, —S—CHF—CF₂Cl, —S—CF₂—CF₂Cl, —S—CFCl—CF₂Cl, —S—CH₂—CH₂—CH₃, —S—CF₂—CF₂—CF₃, —S—CF(CF₃)₂, —S—CH(CH₃)₂ and —S—C(CH₃)₃; R⁵ denotes F; Cl; Br; I; —SF_(S); or denotes a residue selected from the group consisting of methyl, ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, sec-butyl, isobutyl, —C(CH₃)₂(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —O—CH₂—CF₃, —O—C₂F₅, —O—CH₂—CCl₃, —O—CH₂—CBr₃, —O—CHF—CF₂Cl, —O—CF₂—CF₂Cl, —O—CFCl—CF₂Cl, —O—CF₂—CF₂—CF₃, —OCF(CF₃)₂, —OCH(CH₃)₂, —O—C(CH₃)₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S—CH₂—CF₃, —S—C₂F₅, —S—CH₂—CCl₃, —S—CH₂—CBr₃, —S—CHF—CF₂Cl, —S—CF₂—CF₂Cl, —S—CFCl—CF₂Cl, —S—CF₂—CF₂—CF₃, —S—CF(CF₃)₂, —S—CH(CH₃)₂, —S—C(CH₃)₃, —S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F₃, —S(═O)₂—CF₂Cl, —S(═O)₂—CCl₂F, —S(═O)₂—CF₂—CH₃, —S(═O)₂—CH₂—CF₃, —S(═O)₂—C₂F₃—S(═O)₂—CH₂—CCl₃, —S(═O)₂—CH₂—CBr₃, —S(═O)₂—CHF—CF₂Cl, —S(═O)₂—CF₂—CF₂Cl, —S(═O)₂—CFCl—CF₂Cl, —S(═O)₂—CF₂—CF₂—CF₃, —S(═O)₂—CF(CF₃)₂, —S(═O)₂—CH(CH₃)₂ and —S(═O)₂—C(CH₃)₃; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl; T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁵ or T denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁵ or T denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R¹⁰; R⁶ and R⁷, mutually independently, in each case denote H; F; Cl; Br; I; —NO₂; —CN; —C(═O)—OCH₃; —C(═O)—OC₂H₅; or denote a residue selected from the group consisting of —CH₂—OH, methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, n-propyl, isopropyl, sec-butyl, isobutyl and tert-butyl or denote a phenyl residue, which may optionally be substituted in each case with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; R⁸ denotes H; F; Cl; Br; I; —OH; —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—OR²²; or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C(═O)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R⁹ denotes H; F; Cl; Br; I; —NO₂; —CN; or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl and tert-butyl; R¹⁰ denotes —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—OR²²; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂₃—S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²², mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl, cyclohexyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which may optionally be substituted in each case with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R¹² and R¹³ in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, F, Cl, Br, —OH, —CF₃, —SF₅, —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; and R²⁵ and R²⁶, mutually independently, in each case denote a hydrogen residue; denote an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl or denote a residue selected from the group consisting of phenyl, benzyl, phenethyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; providing that R²⁵ and R²⁶ do not in each case denote a hydrogen residue; or R²⁵ and R²⁶ in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; and R³⁰, R³¹ and R³², mutually independently, in each case denote an alkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 11. Compounds according to claim 1, characterized in that X denotes O; Y denotes —NH₂; —NHR³⁰; —NR³¹R³²; denotes an alkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl; n denotes 1; R¹, R³ and R⁴ in each case denote H; R² denotes methyl; —O—CH₃; F; Cl; Br or I; R⁵ denotes a residue selected from the group consisting of methyl, ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂ and —S—CH₂F; T denotes CH and U denotes CH and V denotes N and W denotes C—R⁵ or T denotes CH and U denotes N and V denotes CH and W denotes C—R⁵ or T denotes N and U denotes CH and V denotes CH and W denotes C—R⁵ or T denotes N and U denotes N and V denotes CH and W denotes C—R⁵ or T denotes N and U denotes CH and V denotes N and W denotes C—R⁵ or T denotes CH and U denotes N and V denotes N and W denotes C—R⁵ or T denotes CH and U denotes CH and V denotes CH and W denotes C—R¹⁵; R⁸ denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, pentynyl, butynyl, propynyl, ethynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-Gruppe and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, indolyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R¹⁰ denotes —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; denotes a radical selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a radical selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, indolyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂₃—N(C₂H₅)₂₃—NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂₃—S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R¹¹, R¹², R¹³, R¹⁴ and R¹⁵, mutually independently, in each case denote a radical selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a radical selected from the group consisting of 2,3-dihydro-1H-indenyl, oxetanyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R¹² and R¹³ in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which may optionally in each case be substituted with 1 or 2 substituents mutually independently selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; and R²⁵ denotes an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl or denotes a residue selected from the group consisting of phenyl, benzyl, phenethyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; R²⁶ denotes a hydrogen residue or denote a residue selected from the group consisting of methyl, ethyl and n-propyl; or R²⁵ and R²⁶ in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl n; and R³⁰, R³¹ and R³², mutually independently, in each case denote an alkyl residue selected from the group consisting of —CF₃, —CH₂—CF₃, methyl, ethyl, n-propyl, isopropyl, tert-butyl, n-butyl, sec-butyl and isobutyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 12. Compounds according to claim 1, characterized in that X denotes O or S; n denotes 0, 1 or 2; R¹, R³ and R⁴ in each case denote H; R² denote F; Cl; Br; I or denote a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F; R⁵ denotes F; Cl; Br; I; —SF₅; denotes a residue selected from the group consisting of methyl, ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl; T denotes C—R⁶ and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes N and V denotes C—R⁹ and W denotes C—R⁸ or T denotes N and U denotes C—R⁷ and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes N and V denotes N and W denotes C—R⁸ or T denotes C—R⁶ and U denotes C—R⁷ and V denotes C—R⁹ and W denotes C—R¹⁰; R⁶ and R⁷ in each case denote —CF₃; phenyl; —C(═O)—OCH₃; —C(═O)—OC₂H₅; methyl; —CH₂—OH; H; F; Cl; Br and I; R⁸ denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—OR²²; denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, 4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denote a residue selected from the group consisting of (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R⁹ denotes —CF₃; H; F; Cl; Br or I; R¹⁰ denotes —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; —C(═O)—OR²²; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —ON, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(OH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —ON, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂₃—N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R¹¹, R¹², R¹³, R¹⁴, R¹⁵ and R²², mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —OH₂—OH₂—O—OH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl, 3-pentenyl and tert-butyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R¹² and R¹³ in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which may optionally in each case be substituted with 1 or 2 substituents mutually independently selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, oxo (═O), thioxo (═S), F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —NH₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—CH(CH₃)₂, —C(═O)—C(CH₃)₃, —C(═O)—OH, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂, —C(═O)—O—C(CH₃)₃, —NH—CH₃, —NH—C₂H₅, —NH—C(CH₃)₃, —N(CH₃)₂, —N(C₂H₅)₂, —N(CH₃)(C₂H₅), —NH-phenyl, —N(CH₃)— phenyl, —N(C₂H₅)-phenyl, —N(C₂H₅)-phenyl, —O—CH₂—CH₂—CH₂—CH₃, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, —O-phenyl, —O-benzyl, phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, F, Cl, Br, —OH, —CF₃, —SF_(S), —CN, —NO₂, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, —O—CH₃, —O—C₂H₅, —O—CH(CH₃)₂, —O—C(CH₃)₃, —O—CF₃, —S—CF₃, phenyl and —O-benzyl; and R²⁵ and R²⁶, mutually independently, in each case denote a hydrogen residue; denote an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl or denote a residue selected from the group consisting of phenyl, benzyl, phenethyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; providing that R²⁵ and R²⁶ do not in each case denote a hydrogen residue; or R²⁵ and R²⁶ in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 13. Compounds according to claim 1, characterized in that X denotes O; n denotes 1; R¹, R³ and R⁴ in each case denote H; R² denote methyl; —O—CH₃; F; Cl; Br or I; R⁵ denote a residue selected from the group consisting of methyl, ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂ and —S—CH₂F; or denote a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl; T denotes CH and U denotes CH and V denotes N and W denotes C—R⁸ or T denotes CH and U denotes N and V denotes CH and W denotes C—R⁸ or T denotes N and U denotes CH and V denotes CH and W denotes C—R⁸ or T denotes N and U denotes N and V denotes CH and W denotes C—R⁸ or T denotes N and U denotes CH and V denotes N and W denotes C—R⁸ or T denotes CH and U denotes N and V denotes N and W denotes C—R⁸ or T denotes CH and U denotes CH and V denotes CH and W denotes C—R¹⁰; R⁸ denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a radical selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R¹⁰ denotes —CN; —NH₂; —NO₂; —NHR¹¹; —NR¹²R¹³; —OR¹⁴; —SR¹⁵; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a radical selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂₃—N(C₂H₅)₂₃—NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂₃—S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl substituted; R¹¹, R¹², R¹³, R¹⁴ and R¹⁵, mutually independently, in each case denotes a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denotes a radical selected from the group consisting of 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, oxetanyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denotes a radical selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which may in each case optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R¹² and R¹³ in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which may optionally in each case be substituted with 1 or 2 substituents mutually independently selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[O(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; and R²⁵ denotes an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, methyl, ethyl and n-propyl or denotes a residue selected from the group consisting of benzyl, phenyl, phenethyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; R²⁶ denote a hydrogen residue or denote a residue selected from the group consisting of methyl, ethyl and n-propyl; or R²⁵ and R²⁶ in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 14. Compounds of general formula Ia1 according to claim 1, characterized in that

in which X^(a) denotes O or S; na denotes 0, 1 or 2; R^(2a) denotes F; Cl; Br; I or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F; R^(5a) denotes F; Cl; Br; I; —SF₅; denotes a residue selected from the group consisting of methyl, ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂—(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl; R^(8a) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11a); —NR^(12a)R^(13a); —OR^(14a); —SR^(15a); —C(═O)—OR^(22a); or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—O₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C(═O)—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂₃—NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂₃—S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11a), R^(12a), R^(13a), R^(14a), R^(15a) and R^(22a), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in each case be attached via a —(CH₂)₃—(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃₃—C(═O)—O—C₂H₅₃—C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12a) and R^(13a) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which may optionally in each case be substituted with 1 or 2 substituents mutually independently selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —ON, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; R^(25a) and R^(26a), mutually independently, in each case denote a hydrogen residue; denote a residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl; providing that R^(25a) and R^(26a) do not in each case denote a hydrogen residue; or R^(25a) and R^(26a) in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 15. Compounds of general formula Ia according to claim 14,

in which X^(a), na, R^(5a), R^(8a) and R^(2a) have the meaning as defined in claim 14; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 16. Compounds according to claim 15, characterized in that X^(a) denotes O or S; na denotes 0, 1 or 2; R^(2a) denotes F; Cl; Br; I or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F; R^(5a) denotes F; Cl; Br; I; —SF₅; denotes a residue selected from the group consisting of methyl, ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂—(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃, —S(═O C)₂—CCl₃, —S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl; R^(8a) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11a); —NR^(12a)R^(13a); —OR^(14a); —SR^(15a); —C(═O)—OR^(22a); or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, indolyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂₃—S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11a), R^(12a), R^(13a), R^(14a), R^(15a) and R^(22a), mutually independently, in each case denote a radical from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a radical selected from the group consisting of 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, oxetanyl, cyclopentyl and cyclohexyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12a) and R^(13a) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of


17. Compounds of general formula C1 according to claim 14,

in which na, R^(2a), R^(25a), R^(26a), R^(5a) and X^(a) have the meaning as defined in claim 14; D denotes CH or N; pa denotes 0, qa denotes 0, 1 or 2; Ka, La and Ma, mutually independently, in each case denote H, —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl or sec-butyl; Wa denotes —NR^(34a)R^(35a), —CN, —C(═O)—R^(36a) or —C(═O)—OR^(37a); and R^(34a), R^(35a), R^(36a) and R^(37a), mutually independently, in each case denote H or denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl and isobutyl.
 18. Compounds of general formula C2 according to claim 15,

in which na, R^(2a), R^(5a) and X^(a) have the meaning as defined in claim 15; D denotes CH or N; qa denotes 0, 1 or 2; Ka, La and Ma, mutually independently, in each case denote H, —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl or sec-butyl; and R^(34a) and R^(35a), mutually independently, in each case denote H or denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl and isobutyl.
 19. Compounds of general formula Ib1 according to claim 1,

in which nb denotes 0, 1 or 2; R^(2b) denotes methyl; —O—CH₃; F; Cl; Br or I; R^(8b) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11b); —NR^(12b)R^(13b); —OR^(14b); —SR^(15b); denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; denotes a residue from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-groupand/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂₃—S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11b), R^(12b), R^(13b), R^(14b) and R^(15b), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of oxetanyl, 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denotes a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which may optionally be substituted in each case with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12b) and R^(13b) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which may optionally in each case be substituted with 1 or 2 substituents mutually independently selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; R^(25b) and R^(26b), mutually independently, in each case denote a hydrogen residue; denote an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl; providing that R^(25b) and R^(26b) do not in each case denote a hydrogen residue; or R^(25b) and R^(26b) in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 20. Compounds of general formula Ib according claim 19,

in which nb, R^(8b) and R^(2b) have the meaning as defined in claim 19; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 21. Compounds according to claim 20, characterized in that nb denotes 1; R^(2b) denotes F; R^(8b) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11b); —NR^(12b)R^(13b); —OR^(14b); —SR^(15b); denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or may optionally in each case be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11b), R^(12b), R^(13b), R^(14b) and R^(15b), mutually independently, in each case denote a residue selected from the group consisting of —(CH₂)-pyridinyl, —(CH₂)₂-pyridinyl, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂-β-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, oxetanyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12b) and R^(13b) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which in each case may optionally be substituted with 1 or 2 substituents selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, cyclohexyl, cyclopentyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 22. Compounds of general formula Ic1 according to claim 1,

in which nc denotes 0, 1 or 2; R^(2c) denotes methyl; —O—CH₃; F; Cl; Br or I; R^(8c) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11c); —NR^(12c)R^(13c); —OR^(14c); —SR^(15c); denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, which may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11c), R^(12c), R^(13c), R^(14c) and R^(15c), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—O₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, oxetanyl, cyclopentyl and cyclohexyl, which may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denotes a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12c) and R^(13c) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-aza-spiro[2.5]octyl, 3-aza-aza-bicyclo[3.2.1]octyl, 6-aza-aza-bicyclo[3.3.1]heptyl, 8-aza-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which in each case may optionally be substituted with 1 or 2 substituents selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂₃—N(C₂H₅)₂₃—NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; R^(25c) and R^(26c), mutually independently, in each case denote a hydrogen residue; or denote a residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl; providing that R^(25c) and R^(26c) do not in each case denote a hydrogen residue; or R^(25c) and R^(26c) in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 23. Compounds of general formula Ic according claim 22,

in which nc, R^(8c) and R^(2c) have the meaning as defined in claim 22; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 24. Compounds according to claim 23, characterized in that nc denotes 1; R^(2c) denotes F; R^(8c) denotes H; F; Cl; Br; I; —CN; —OH; —NH₂; —NO₂; —NHR^(11c); —NR^(12c)R^(13c); —OR^(14c); —SR^(15c); denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, ethyl, —CF₂—CH₃, —CH₂—CF₃, —C₂F₅, —CH₂—CCl₃, —CH₂—CBr₃, —CHF—CF₂Cl, —CF₂—CF₂Cl, —CFCl—CF₂Cl, n-propyl, —CF₂—CF₂—CF₃, —CF(CF₃)₂, isopropyl, sec-butyl, isobutyl, tert-butyl, —CH₂—CH₂—CH₂—CF₃, —CH₂—CH₂—CH₂—CH₂—CF₃, —CH₂—C(═O)—O—CH₃, —CH₂—C(═O)—C₂H₅, —CH₂—C(═O)—C(CH₃)₃, —CH₂—O—C(═O)—CH₃, —CH₂—O—C(═O)—C₂H₅, —CH₂—O—C(═O)—CH(CH₃)₂, —CH₂—O—C(═O)—C(CH₃)₃, n-butyl, n-pentyl, n-hexyl, (3,3)-dimethyl-but-1-yl, 3-methyl-but-1-yl, 4-methyl-pent-1-yl, (3,3)-dimethyl-but-1-ynyl, 4-methyl-pent-1-ynyl, 1-hexynyl, propynyl, ethynyl, butynyl, pentynyl, 2-methyl-propen-1-yl, 3-methyl-but-2-en-1-yl, 1-pentenyl, 1-octenyl, 1-heptenyl, 1-hexenyl and (3,3)-dimethyl-but-1-enyl; denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, wherein the residue may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11c), R^(12c), R^(13c), R^(14c) and R^(15c), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, oxetanyl, cyclopentyl and cyclohexyl, wherein the residue may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denotes a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12c) and R^(13c) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which in each case may optionally be substituted with 1 or 2 substituents selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 25. Compounds of general formula Id1 according to claim 1,

in which X^(d) denotes O or S; nd denotes 0, 1 or 2; R^(2d) denotes F; Cl; Br; I or denotes a residue selected from the group consisting of methyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —O—CH₃, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —S—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl and —S—CCl₂F; R^(5d) denotes F; Cl; Br; I; —SF₅; denotes a residue selected from the group consisting of methyl, ethyl, —CF₃, —CCl₃, —CBr₃, —CHF₂, —CH₂F, —CF₂Cl, —CCl₂F, —C(CH₃)₂—(CH₂OH), tert-butyl, —O—CF₃, —O—CCl₃, —O—CBr₃, —O—CHF₂, —O—CH₂F, —O—CF₂Cl, —O—CCl₂F, —O—CF₂—CH₃, —S—CF₃, —S—CCl₃, —S—CBr₃, —S—CHF₂, —S—CH₂F, —S—CF₂Cl, —S—CCl₂F, —S—CF₂—CH₃, —S(═O)₂—CF₃, —S(═O)₂—CCl₃, —S(═O)₂—CBr₃, —S(═O)₂—CHF₂, —S(═O)₂—CH₂F and —S(═O)₂—CF₂Cl; or denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopentenyl and cyclohexenyl; R^(10d) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11d); —NR^(12d)R^(13d); —OR^(14d); —SR^(15d); —C(═O)—OR^(22d); denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, indolyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, wherein the residue may in each case be attached via a —(CH═CH)—, —C═C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF₅, —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11d), R^(12d), R^(13d), R^(14d), R^(15d), and R^(22d), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, oxetanyl, cyclopentyl and cyclohexyl, wherein the residue may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denotes a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12d) and R^(13d) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which in each case may optionally be substituted with 1 or 2 substituents selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; R^(25d) and R^(26d), mutually independently, in each case denote a hydrogen residue; or denote an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl; providing that R^(25d) and R^(26d) do not in each case denote a hydrogen residue; or R^(25d) and R^(26d) in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 26. Compounds of general formula Id according to claim 25,

in which X^(d), nd, R^(2d), R^(5d) and R^(10d) have the meaning as defined in claim 25; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 27. Compounds of general formula Ie1 according to claim 1,

in which ne denotes 0, 1 or; R^(2e) denotes methyl; —O—CH₃; F; Cl; Br or I; R^(10e) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11e); —NR^(12e)R^(13e); —OR^(14e); —S^(15e); denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, wherein the residue may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11e), R^(12e), R^(13e), R^(14e) and R^(15e), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of oxetanyl, 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, wherein the residue may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12e) and R^(13e) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which in each case may optionally be substituted with 1 or 2 substituents selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)— phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; R^(25e) and R^(26e), mutually independently, in each denote a hydrogen residue; or denote an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl; providing that R^(25e) and R^(26e) do not in each case denote a hydrogen residue; or R^(25e) and R^(26e) in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 28. Compounds of general formula Ie according to claim 27,

in which ne, R^(10e) and R^(2e) have the meaning as defined in claim 27, in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 29. Compounds according to claim 28, characterized in that ne denotes 1; R^(2e) denotes F; R^(10e) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11e); —NR^(12e)R^(13e); —OR^(14e); —SR^(15e); denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of tetrazolyl, (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, wherein the residue may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11e), R^(12e), R^(13e), R^(14e) and R^(15e), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of oxetanyl, 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, wherein the residue may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12e) and R^(13e) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which in each case may optionally be substituted with 1 or 2 substituents selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 30. Compounds of general formula If1 according to claim 1,

in which nf denotes 0, 1 or 2; R^(2f) denotes methyl; —O—CH₃; F; Cl; Br or I; R^(10f) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11f); —NR^(12f)R^(13f); —OR^(14f); —SR^(15f); denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, wherein the residue may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11f), R^(12f), R^(13f), R^(14f) and R^(15f), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of oxetanyl, 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, wherein the residue may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denote a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12f) and R^(13f) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which in each case may optionally be substituted with 1 or 2 substituents selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)— phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; R^(25f) and R^(26f), mutually independently, in each case denote a hydrogen residue; or denote an alkyl residue selected from the group consisting of —CH₂—OH, —CH₂—CH₂—OH, —CH₂—CH₂—CH₂—OH, —CH₂—CH₂—CH₂—CH₂—OH, isopropyl, n-butyl, sec-butyl, isobutyl, methyl, ethyl and n-propyl; providing that R^(25f) and R^(26f) do not in each case denote a hydrogen residue; or R^(25f) and R^(26f) in each case together with the carbon atom joining them together as a ring member, form a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 31. Compounds of general formula If according to claim 30,

in which nf, R^(10f) and R^(2f) have the meaning as defined in claim 30; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 32. Compounds according to claim 31, characterized in that nf denotes 1; R^(2f) denotes F; R^(10f) denotes —CN; —OH; —NH₂; —NO₂; —NHR^(11f); —NR^(12f)R^(13f); —OR^(14f); —SR^(15f); denotes a residue selected from the group consisting of cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclohexenyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, azepanyl, diazepanyl, azocanyl and thiomorpholinyl, which is in each case attached to the parent structure via a carbon atom of the rings of the above-stated residues or via a —(CH═CH)—, —C≡C— or —C≡C—CH₂-group and in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, oxo (═O), thioxo (═S), methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl and n-pentyl; or denotes a residue selected from the group consisting of (1,3)-benzodioxolyl, (1,4)-benzodioxanyl, indolyl, tetrazolyl, (2,3)-dihydrothieno[3,4-b][1,4]dioxinyl, benzo[b]furanyl, phenyl, naphthyl, oxazolyl, thiazolyl, imidazolyl, pyrimidinyl, thiophenyl, furanyl and pyridinyl, wherein the residue may in each case be attached via a —(CH═CH)—, —C≡C—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of F, Cl, Br, I, —CN, —CF₃, —SF_(S), —OH, —O—CH₃, —O—C₂H₅, —NH₂, —N(CH₃)₂, —N(C₂H₅)₂, —NH—S(═O)₂—CH₃, —NH—S(═O₂)—C₂H₅, —NH—S(═O)₂—CH(CH₃)₂, —NO₂, —O—CF₃, —S—CF₃, —SH, —S—CH₃, —S—C₂H₅, —S—CH(CH₃)₂, —S—C(CH₃)₃, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; R^(11f), R^(12f), R^(13f), R^(14f) and R^(15f), mutually independently, in each case denote a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; denote a residue selected from the group consisting of oxetanyl, 2,3-dihydro-1H-indenyl, piperidinyl, pyrrolidinyl, cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl, wherein the residue may in each case be attached via a —CH₂—O—, —CH₂—CH₂—O—, —CH₂—CH₂—O—CH₂—, —CH₂—CH(CH₃)—O—CH₂—, —(CH₂)—, —(CH₂)₂— or —(CH₂)₃-group and/or in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, n-pentyl, n-hexyl, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—CH(CH₃)₂ and —C(═O)—O—C(CH₃)₃; or denotes a residue selected from the group consisting of —(CH₂)— pyridinyl, —(CH₂)₂-pyridinyl, benzyl, phenethyl, phenyl, naphthyl, thiophenyl, furanyl, pyrrolyl and pyridinyl, which in each case may optionally be substituted with 1, 2, 3, 4 or 5 substituents selected from the group consisting of —CF₃, F, Cl, Br, —O—CH₃, —O—C₂H₅, methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl and tert-butyl; or R^(12f) and R^(13f) in each case together with the nitrogen atom joining them together as a ring member, form a residue selected from the group consisting of 3-aza-bicyclo[3.1.1]heptyl, 6-aza-spiro[2.5]octyl, 3-aza-bicyclo[3.2.1]octyl, 6-aza-bicyclo[3.3.1]heptyl, 8-aza-bicyclo[3.2.1]octyl, 1-oxa-2,8-diaza-spiro[4.5]dec-2-enyl, azocanyl, isoindolyl, indolyl, (1,2,3,6)-tetrahydropyridinyl, (4,5,6,7)-tetrahydroisoxazolo[5,4-c]pyridinyl, pyrrolidinyl, piperidinyl, (1,2,3,6)-tetrahydropyridinyl, piperazinyl, morpholinyl, azepanyl, diazepanyl and thiomorpholinyl, which in each case may optionally be substituted with 1 or 2 substituents selected from the group consisting of —CH₂—O—CH₂-oxetanyl, —O—CH₂-oxetanyl, —CH₂—OH, —CH₂—CH₂—OH, ═CH₂, —C(═O)—O—CH₃, —C(═O)—O—C₂H₅, —C(═O)—O—C(CH₃)₃, —C(═O)—CH₃, —C(═O)—C₂H₅, —C(═O)—C(CH₃)₃, —CN, —CH₂—N(CH₃)₂, —CH₂—N(C₂H₅)₂, —CH₂—NH—CH₃, —CH₂—NH—C₂H₅, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, —CH₂—O—CH₃, —CH₂—O—CH₂—CH₃, —CH₂—O—CH₃, —NH₂, —NH—CH₃, —NH—C₂H₅, —N(CH₃)₂, —N(C₂H₅)₂, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, oxo (═O), thioxo (═S), —OH, F, Cl, Br, —CF₃, —O—CH₃, —O—C₂H₅, —O—C(CH₃)₃, —O—CH(CH₃)₂, —O—CH₂—CH₂—CH₂—CH₃, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl, sec-butyl, piperidinyl, pyrrolidinyl, —O-phenyl, —O—C(═O)—CH₃, —O—C(═O)—C₂H₅, —O—C(═O)—C(CH₃)₃, —(CH₂)-pyridinyl, cyclohexyl, cyclopentyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, pyridinyl, phenyl and benzyl, wherein in each case the cyclic moiety of the residues oxetanyl, —N—[C(═O)—C₂H₅]-phenyl, —N—[C(═O)—CH₃]-phenyl, (4,5)-dihydroisoxazolyl, thiazolyl, (1,2,5)-thiadiazolyl, thiophenyl, phenethyl, —NH-phenyl, —N(CH₃)-phenyl, —N(C₂H₅)-phenyl, —(CH₂)-pyridinyl, pyridinyl, phenyl, —O-phenyl and benzyl may optionally be substituted with 1, 2, 3, 4 or 5 substituents mutually independently selected from the group consisting of —CF₃, —OH, —O—CH₃, —O—C₂H₅, F, Cl, Br, methyl, ethyl, isopropyl, n-propyl, n-butyl, tert-butyl and sec-butyl; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 33. Compounds of general formula Ig according to claim 1,

in which ng denotes 0, 1 or 2; R^(2g) denotes methyl; —O—CH₃; F; Cl; Br or I; R^(14g) denotes a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; T denotes CH and U denotes N and V denotes CH or T denotes N and U denotes CH and V denotes CH or T denotes N and U denotes N and V denotes CH or T denotes N and U denotes CH and V denotes N or T denotes CH and U denotes N and V denotes N; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 34. Compounds according to claim 33, characterized in that ng denotes 1; R^(2g) denotes F; R^(14g) denotes a residue selected from the group consisting of methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, 3-pentyl, n-heptyl, 4-heptyl, n-octyl, n-nonyl, 5-nonyl, (2,6)-dimethyl-hept-4-yl, 3-methyl-butyl, n-hexyl, (3,3)-dimethylbutyl, —CH₂—CH₂—O—CH₃, —CH₂—CH₂—O—C₂H₅, —CH₂—CH₂—O-phenyl, —CH₂—CH₂—CH₂—O—CH₃, ethenyl, propenyl, 2-butenyl, 3-butenyl, 2-pentenyl and 3-pentenyl; T denotes CH and U denotes N and V denotes CH or T denotes N and U denotes CH and V denotes CH or T denotes N and U denotes N and V denotes CH or T denotes N and U denotes CH and V denotes N or T denotes CH and U denotes N and V denotes N; in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 35. Compounds according to claim 1 selected from the group consisting of [1] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-methyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [2] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [3]2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [4] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-fluoro-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [5] N-((2-chloro-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [6] N-((-bromo2-bromo-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [7] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-iodo-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [8] N-((2-tert-butyl-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [9] N-((2-cyano-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [10] (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [11] (R)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [12] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-morpholino-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [13] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [14] N-((2-(dimethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [15] N-((2-(diethylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [16] N-((2-(dipropylamino)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [17] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-hydroxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [18] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-methoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [19] N-((2-butoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [20] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-isopropoxy-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [21] N-((2-cyclopentyloxy-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonam ido)phenyl)propanamide [22] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-phenyl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [23] 2-(3-fluoro-4-(methylsulfonam ido)phenyl)-N-((2-(4-fluoro-phenyl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [24] 2-(3-fluoro-4-(methylsulfonam ido)phenyl)-N-((6-(trifluoromethyl)-2,2′-bipyridin-3-yl)methyl)propanamide [25] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((6-(trifluoromethyl)-2,3′-bipyridin-3-yl)methyl)propanamide [26] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pyrimidin-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [27] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(thiazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [28] 2-(3-fluoro-4-(methylsulfonam ido)phenyl)-N-((2-(oxazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [29] N-((2-(1H-imidazol-2-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [30] N-(2-cyano-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [31] (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [32] (R)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [33] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-morpholino-4-(trifluoromethyl)benzyl)propanamide [34] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [35] N-(2-(dimethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [36] N-(2-(diethylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [37] N-(2-(dipropylamino)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [38] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-hydroxy-4-(trifluoromethyl)benzyl)propanamide [39] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-methoxy-4-(trifluoromethyl)benzyl)propanamide [40] N-(2-butoxy-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [41] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-isopropoxy-4-(trifluoromethyl)benzyl)propanamide [42] N-(2-(cyclopentyloxy)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [43] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide [44] 2-(3-fluoro-4-(methylsulfonam ido)phenyl)-N-((4′-fluoro-5-(trifluoromethyl)biphenyl-2-yl)methyl)propanamide [45] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-2-yl)-4-(trifluoromethyl)benzyl)propanamide [46] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyridin-3-yl)-4-(trifluoromethyl)benzyl)propanamide [47] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(pyrimidin-2-yl)-4-(trifluoromethyl)benzyl)propanamide [48] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(thiazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide [49] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(oxazol-2-yl)-4-(trifluoromethyl)benzyl)propanamide [50] N-(2-(1H-imidazol-2-yl)-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [51] N-((6-tert-butyl-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [52] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((4-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [53] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((3-(piperidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide [54] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((4-(piperidin-1-yl)-2-(trifluoromethyl)pyrimidin-5-yl)methyl)propanamide [55] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((3-(piperidin-1-yl)-5-(trifluoromethyl)pyrazin-2-yl)methyl)propanamide [56] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((4-(piperidin-1-yl)-6-(trifluoromethyl)pyridazin-3-yl)methyl)propanamide [57] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)propanamide [58] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperidin-1-yl)-4-(trifluoromethyl)phenyl)propanamide [59] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)ethyl)propanamide [60] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)phenethyl)propanamide [61] N-(2-amino-4-(trifluoromethyl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [62] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-nitro-4-(trifluoromethyl)benzyl)propanamide [63] N-(4-tert-butyl-2-(piperidin-1-yl)benzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [64] 2-(3-chloro-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [65] 2-(3-chloro-4-(methylsulfonamido)phenyl)-N-((2-(pyrrolidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [66] 2-(3-chloro-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [67] 2-(3-bromo-4-(methylsulfonamido)phenyl)-N-((2-(piperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [68] 2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(piperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [69] 2-(3-bromo-4-(methylsulfonamido)phenyl)-N-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide [70] N-(4-tert-butyl-2-cyanobenzyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [71] N-((6-(chlorodifluoromethyl)-2-(piperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-(4-methylsulfonamido)phenyl)propanamide [72] (S)-2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-morpholino-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [73] N-((2-(4-benzylpiperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [74] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-piperazin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide; [76] N-((2-(cyclohexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl-2-(3-fluoro-4-methylsulfonamido)phenyl)propanamide [77] N-((3-chloro-5-(trifluoromethyl)pyridin-2-yl)methyl-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [78] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((3-(pyrrolidin-1-yl)-5-(trifluoromethyl)pyridin-2-yl)methyl)propanamide [79] N-((2-(3,5-dimethylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [80] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide [81] N-((2-(azepan-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide [82] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-(2-(4-methylpiperidin-1-yl)-4-(trifluoromethyl)benzyl)propanamide; 83 (S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-propionamide 84 (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-propionamide 85 N-(2-dimethylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 87 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-imidazol-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 88 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-thiophen-2-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 89 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 90 N-(2-cyclohexylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 91 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 93 (S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 94 (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 95 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 96 (S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 97 (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 98 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-4-trifluoromethyl-benzyl)-propionamide 99 (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-isobutoxy-4-trifluoromethyl-benzyl)-propionamide 100 N-(2-cyclopropylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 101 N-(2-cyclobutylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 102 2-(3-chloro-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 103 2-(3-bromo-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 104 N-(4-benzyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 106 N-(2-benzyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 107 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methoxy-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 108 N-(2-butoxy-4-tert-butyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 109 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 110 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 111 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-propoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 112 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 113 N-[2-(4-chloro-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 114 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-fluoro-4-trifluoromethyl-benzyl)-propionamide 115 N-(2-benzylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 116 N-(2-butylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 117 N-[2-(4-tert-butyl-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 118 N-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 120 (S)—N-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 121 (R)—N-[2-(3-chloro-4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 122 N-(2-butylsulfanyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 123 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 124 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-methyl-cyclopropylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 125 N-[2-(3,3-dimethyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 126 N-(2-cyclohexylsulfanyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 127 2-(4-methylsulfonamido-3-methyl-phenyl)-N-(6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 128 N-(2-azocan-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 129 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pyrrolidin-1-yl-4-trifluoromethyl-benzyl)-thiopropionamide 130 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-thiopropionamide 131 N-[6′-(chloro-difluoro-methyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 132 N-[2-azepan-1-yl-6-(chlor-difluor-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 133 N-(4-tert-butyl-2-isobutoxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 134 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 135 N-[2-(3,4-dimethyl-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 136 N-[2-(5-chloro-2-methyl-phenylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 137 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 138 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-fluoro-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 139 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 140 N-[2-butoxy-6-(chlor-difluor-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 142 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 144 (S)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 145 (R)-2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 147 N-[2-(4-chloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 148 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 149 N-[2-(3-chloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 150 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 151 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 152 N-[4-tert-butyl-2-(2,2-dimethyl-propoxy)-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 153 N-(4-tert-butyl-2-pentyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 154 N-(4-tert-butyl-2-cyclohexyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 155 N-(4-tert-butyl-2-cyclopentyloxy-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 156 N-(2-cyclobutoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 157 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 158 acetic acid-3′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-ylester 159 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 160 N-(4-butoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 161 N-(2-cyclopentylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 162 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-isopropoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 163 N-(2-ethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 164 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6″-trifluoromethyl-3,4,5,6,3′,4′,5′,6′-octahydro-2H,2′H-[1,4′;1′,2″]terpyridin-3″-ylmethyl)-propionamide 165 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-pyrrolidin-1-yl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 166 N-[6-(chloro-difluoro-methyl)-2-cyclopentyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 167 N-[2-(butyl-methyl-amino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 168 N-[6-(chloro-difluoro-methyl)-2-cyclohexyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 169 N-[2-benzyloxy-6-(chlor-difluor-methyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 170 N-[2-(4-tert-butyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 171 N-[2-(4-ethyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 172 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 173 N-[2-(4-chloro-benzylamino)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 174 N-(2-azepan-1-yl-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 175 N-[2-(4-fluoro-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 176 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-pyridin-4-yl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 177 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-4-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 178 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenethyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 179 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide 180 N-[6-(chloro-difluoro-methyl)-2-hexyloxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 181 N-[6-(chloro-difluoro-methyl)-2-(pyridin-3-ylmethoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 182 N-[6-(chloro-difluoro-methyl)-2-(pyridin-2-ylmethoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 183 N-(2-dibutylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 184 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6′-(4-fluoro-phenyl)-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide 185 N-[2-azepan-1-yl-6-(4-fluoro-phenyl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 186 N-[6-(chloro-difluoro-methyl)-2-dipropylamino-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 187 N-[6′-(chloro-difluoro-methyl)-3,5-dimethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 188 N-[2-(1,3-dihydro-isoindol-2-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 189 3′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-carbonic acid ethylester 190 N-(4,6′-bis-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 191 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-styryl-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide 192 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenethyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 193 N-{2-[4-(3-chloro-pyridin-2-yl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 194 N-{2-[4-(3-chloro-pyridin-2-yl)-2-methyl-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 195 N-(4,6′-bis-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide 196 2-(4-methylsulfonamido-3-methyl-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 197 N-(4-ethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 198 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-phenoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 199 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methoxymethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 200 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide 201 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(2-fluoro-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide 202 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-2-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 203 2-(4-methylsulfonamido-3-methyl-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 204 N-(2-benzyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide 205 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(methyl-phenyl-amino)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 206 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-trifluoromethyl-2-(4-trifluoromethyl-benzyloxy)-benzyl]-propionamide 207 N-[6-(chloro-difluoro-methyl)-2-(4-phenyl-piperazin-1-yl)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 208 N-[6-(chloro-difluoro-methyl)-2-isobutoxy-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 209 N-(2-benzyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 210 N-(4,4-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 211 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(pyridin-3-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 212 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(3-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-pyridin-3-ylmethyl}-propionamide 213 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(3-trifluoromethyl-pyridin-2-yl)-piperazin-1-yl]-pyridin-3-ylmethyl}-propionamide 214 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-pyridin-2-yl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 215 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 216 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-phenyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide 217 N-(2-azocan-1-yl-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 218 N-[2-(4,4-dimethyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 219 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-p-tolyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 220 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-m-tolyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 221 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide 222 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{6-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-pyridin-3-ylmethyl}-propionamide 223 N-(2-benzyloxy-4-hydroxymethyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 225 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pentyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 226 2,2-dimethyl-propionic acid-3′-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-4-yl ester 227 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-oxo-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 228 N-(4-ethoxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 229 N-[2-(4-ethyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 230 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-trifluoromethyl-2-(4-trifluoromethyl-piperidin-1-yl)-benzyl]-propionamide 231 N-[2-(4-benzyl-piperidin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 233 N-(6-tert-butyl-2-cyclohexyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 234 N-(6-tert-butyl-2-cyclopentyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 235 N-(2-butoxy-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 236 N-(6-tert-butyl-2-hexyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 237 N-(2-benzyloxy-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 238 N-(2-cyclohexyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 239 (R)—N-(2-cyclohexyloxy-4-trifluoromethyl-benzyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 240 N-(6-tert-butyl-2-pyrrolidin-1-yl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 241 N-(6′-tert-butyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 242 N-[2-(4-ethyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 243 N-[2-(4-butyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 244 N-[2-(4-tert-butyl-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 245 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(indan-2-yloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 246 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-p-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide 247 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-m-tolyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-propionamide 248 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{4-trifluoromethyl-2-[4-(4-trifluoromethyl-phenyl)-piperazin-1-yl]-benzyl}-propionamide 249 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-methoxy-phenyl)-piperazin-1-yl]-4-trifluoromethyl-benzyl}-propionamide 250 N-[2-(3,4-dichloro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 251 N-[2-(3-tert-butyl-1-oxa-2,8-diaza-spiro[4.5]dec-2-en-8-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 252 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-phenyl-1-oxa-2,8-diaza-spiro[4.5]dec-2-en-8-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 253 2-(3-fluoro-4-(pentafluorsulfanylsulfonamido)phenyl)-N-p-tolylpropanamid 254 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-fluoro-4-methoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 255 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[4-(4-fluoro-phenyl)-piperidin-1-yl]-4-trifluoromethyl-benzyl}-propionamide 256 N-(2-butoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide 257 N-(2-hexyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide 258 N-[2-(4-chloro-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 259 N-(4-dimethylaminomethyl-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 260 N-[2-(4-cyclohexyl-piperazin-1-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 261 N-(6-tert-butyl-2-cyclopentyloxy-4-hydroxymethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 262 2-(4-methylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 263 N-[2-(3,3-dimethyl-butyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 264 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-p-tolyl-ethyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 265 N-[2-(2,3-dihydro-benzo[1,4]dioxin-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 266 N-(2-benzo[1,3]dioxol-5-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 267 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 268 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-pentyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 269 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-hydroxy-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 270 N-(2-cyclohexylmethoxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 271 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-cyclohexylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 272 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methylsulfonamido-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 273 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-methyl-propenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 274 N-[2-(3,3-dimethyl-but-1-enyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 275 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1H-indol-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 276 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1H-indol-5-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 277 N-[2-(4-chloro-3-fluoro-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 278 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-fluoro-3-methyl-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 279 N-[2-(2,2-dimethyl-cyclopropylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonam ido-phenyl)-propionamide 282 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(3-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 283 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 284 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-yl)-ethyl]-propionamide 285 N-(4-cyano-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 287 2-(4-ethanesulfonylamino-3-fluoro-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 288 2-(4-(N,N-dimethylsulfamoylamino)-3-fluorphenyl)-N-((2-(4-methylpipendin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide 289 2-(4-methylsulfonamido-3-methoxy-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 290 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenylamino-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 291 N-(2-cyclohexyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 292 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 293 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-thiopropionamide 294 N-(2-cyclohexylsulfanyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 295 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 296 N-(2-azepan-1-yl-6-tert-butyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 297 N-(6-tert-butyl-2-dipropylamino-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 298 N-(2-but-2-enyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 299 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-2-enyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 300 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 301 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-pent-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 302 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-hexyloxy-4-methyl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 303 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-{2-[2-(4-fluoro-phenyl)-ethyl]-6-trifluoromethyl-pyridin-3-ylmethyl}-propionamide 304 N-(4-acetyl-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 307 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(phenyl-propionyl-amino)-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide 308 N-[2-(4-dimethylamino-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 309 2-[3-fluoro-4-(propan-2-sulfonylamino)-phenyl]-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 310 2-[3-fluoro-4-(2,2,2-trifluor-ethansulfonylamino)-phenyl]-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 311 N-[2-(2,6-dimethyl-morpholin-4-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 312 2-(3-fluoro-4-trifluormethylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 313 2-(3-fluoro-4-(sulfamoylamino)phenyl)-N-((2-(4-methylpiperidin-1-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide 314 N-[2-(1,1-dioxo-1,6-thiomorpholin-4-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 315 N-(6′-difluormethyl-4-methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 316 N-(4,6′-dimethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 317 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-phenyl-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 318 N-(4,4′-dimethyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 319 N-[2-(4-cyclohexyl-piperazin-1-yl)-4-trifluoromethyl-benzyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 320 N-(4′-tert-butyl-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 321 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4′-methoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-propionamide 322 N-(3′-chloro-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 323 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(3′-fluoro-5-trifluoromethyl-biphenyl-2-ylmethyl)-propionamide 324 N-(3′-chloro-4′-fluoro-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 325 N-(3′,4′-dimethoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 326 N-[2-(3,4-dimethoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 327 4-(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-yloxymethylypiperidine-1-carbonic acid tert-butyl ester 328 N-(6-tert-butyl-2-pentyloxy-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 329 N-[6-tert-butyl-2-(3-methyl-butoxy)-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 330 N-(4-dimethylamino-4-phenyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 331 N-(2-dipropylamino-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(4-methylsulfonamido-3-methyl-phenyl)-propionamide 332 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[4-(4-fluoro-phenyl)-6′-trifluoromethyl-3,6-dihydro-2H-[1,2′]bipyridinyl-3′-ylmethyl]-propionamide 334 N-(2-cyclohex-1-enyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 335 N-[2-(1-ethyl-propoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 336 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1-propyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 337 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(1-isobutyl-3-methyl-butoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 338 N-[2-(4,4-dimethyl-cyclohexyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 339 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6-trifluoromethyl-2-(4-trifluoromethyl-cyclohexyloxy)-pyridin-3-ylmethyl]-propionamide 340 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[6-trifluoromethyl-2-(4-trifluoromethyl-cyclohexyloxy)-pyridin-3-ylmethyl]-propionamide 341 4-(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-yloxyypiperidine-1-carbonic acid tert-butyl ester 342 4-[(3-{[2-(3-fluoro-4-methylsulfonamido-phenyl)-propionylamino]-methyl}-6-trifluoromethyl-pyridin-2-ylaminoymethyl]-piperidine-1-carbonic acid tert-butyl ester 343 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(piperidin-4-ylmethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 344 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(piperidin-4-yloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 345 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(2-p-tolyloxy-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide 346 N-[2-(2-cyclohexyl-vinyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 347 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methyl-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-butyramide 348 N-[2-(3,5-dimethoxy-phenyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 349 N-(2-cyclopentyloxy-4-methyl-6-trifluoromethyl-pyridin-3-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 350 N-(3′,5-dimethoxy-5-trifluoromethyl-biphenyl-2-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 351 ethyl 5-((2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamido)methyl)-6-(4-methylpiperidin-1-yl)-2-(trifluoromethyl)nicotinat 352 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(nonan-5-yloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide 353 N-((6-tert-butyl-2-isobutoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide 354 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(phenylethynyl)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide 355 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(3-methoxypropoxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide 356 N-((2-(4-benzylpiperidin-1-yl)-4-methyl-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide 357 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-methylene-6′-trifluoromethyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 358 N-[2-(6-aza-spiro[2.5]oct-6-yl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 359 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(3-methyl-but-2-enyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 360 N-[2-(3-cyclohexyl-propyl)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 361 N-[2-(3-ethoxy-propoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 362 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-[2-(2-phenoxy-ethoxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-propionamide 363 N-[2-(3,5-dimethoxy-benzyloxy)-6-trifluoromethyl-pyridin-3-ylmethyl]-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 364 2-(3-fluoro-4-methylsulfonamido-phenyl)-N-(4-hydroxymethyl-6′-trifluoro methyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-propionamide 365 N-(6′-tert-butyl-4-phenyl-3,4,5,6-tetrahydro-2H-[1,2′]bipyridinyl-3′-ylmethyl)-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 366 N-{6-tert-butyl-2-[4-(4-fluoro-phenyl)-piperazin-1-yl]-pyridin-3-ylmethyl}-2-(3-fluoro-4-methylsulfonamido-phenyl)-propionamide 367 2-(4-methylsulfonamido-3-methyl-phenyl)-N-(2-pyrrolidin-1-yl-6-trifluoromethyl-pyridin-3-ylmethyl)-propionamide [368] N-((2-(1H-indol-4-yl)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [369] N-((6-tert-butyl-2-propoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [370] N-((6-tert-butyl-2-(3-methoxypropoxy)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [371] N-((6-tert-butyl-2-(4-(dimethylamino)-4-phenylpiperidin-1-yl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [372] N-((6-tert-butyl-2-methoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [373] N-((6-tert-butyl-2-ethoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [374] N-((6-tert-butyl-2-isopropoxypyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [375] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(pentyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide, [376] 2-(3-fluoro-4-(methylsulfonamido)phenyl)-N-((2-(hexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)propanamide, [377] N-((2-(3,5-dimethylcyclohexyloxy)-6-(trifluoromethyl)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, [378] N-((6-tert-butyl-2-(2-ethoxyethoxy)pyridin-3-yl)methyl)-2-(3-fluoro-4-(methylsulfonamido)phenyl)propanamide, in each case optionally in the form of one of the pure stereoisomers thereof, in particular enantiomers or diastereomers, the racemates thereof or in the form of a mixture of stereoisomers, in particular the enantiomers and/or diastereomers, in any desired mixing ratio, or in each case in the form of corresponding salts or in each case in the form of corresponding solvates.
 36. Compounds according to claim 1, characterized in that, in an FLIPR assay with CHO-K21 cells which have been transfected with the human gene VR1, in a concentration of less than 2000 nM, preferably of less than 1000 nM, particularly preferably of less then 300 nM, very particularly preferably of less than 100 nM, still more preferably of less than 75 nM, even more preferably of less than 50 nM, most preferably of less than 10 nM; effect 50% displacement of capsaicin which is present in a concentration of 100 nM.
 37. A process for the production of a compound according to claim 1, characterized in that at least one compound of the general formula II,

in which R⁵, U, T, V and W have the meaning according to claim 1, m denotes 0, 1, 2 or 3 and R denotes or denotes a C₁₋₆ alkyl residue, is reacted in a reaction medium, in the presence of at least one reducing agent, preferably in the presence of at least one reducing agent selected from the group consisting of sodium hydride, sodium, potassium hydride, lithium aluminum hydride, sodium borohydride and di(isobutyl)aluminum hydride, to yield at least one compound of the general formula III,

in which R⁵, U, T, V and W have the meaning according to claim 1 and m denotes 0, 1, 2 or 3 and said compound is optionally purified and/or isolated, and at least one compound of the general formula III is reacted in a reaction medium in the presence of diphenylphosphoryl azide or in the presence of HN₃ to yield at least one compound of the general formula IV,

in which R⁵, U, T, V and W have the meaning according to claim 1 and m denotes 0, 1, 2 or 3 and said compound is optionally purified and/or isolated, and at least one compound of the general formula IV is reacted in a reaction medium in the presence of at least one reducing agent, preferably in the presence of at least one reducing agent selected from the group consisting of sodium hydride, potassium hydride, lithium aluminum hydride, sodium borohydride and di(isobutyl)aluminum hydride or in a reaction medium in the presence of a catalyst, preferably in the presence of a catalyst is based on platinum or palladium, particularly preferably in the presence of palladium on carbon, and in the presence of hydrogen or in the presence of hydrazine or in a reaction medium in the presence of triphenylphosphine to yield at least one compound of the general formula V,

in which R⁵, U, T, V and W have the meaning according to claim 1 and m denotes 0, 1, 2 or 3 and said compound is optionally purified and/or isolated, or at least one compound of the general formula VI,

in which R⁵, U, T, V, and W have the meaning according to claim 1 and m denotes 0, 1, 2 or 3, is reacted in a reaction medium in the presence of at least one catalyst, preferably in the presence of at least one catalyst based on palladium or platinum, particularly preferably in the presence of palladium on carbon, optionally in the presence of at least one acid, preferably in the presence of hydrochloric acid, or in the presence of at least one reducing agent selected from the group consisting of BH₃.S(CH₃)₂, lithium aluminum hydride and sodium borohydride, optionally in the presence of NiCl₂, to yield at least one compound of the general formula V, optionally in the form of a corresponding salt, preferably in the form of a corresponding hydrochloride, and said compound is optionally purified and/or isolated, and at least one compound of the general formula V is reacted with at least one compound of the general formula VII,

in which Y, R¹, R², R³, R⁴, R²⁵ and R²⁶ have the meaning according to claim 1, in a reaction medium, optionally in the presence of at least one suitable coupling agent, optionally in the presence of at least one base, or with at least one compound of the general formula VIII,

in which Y, R¹, R², R³, R⁴, R²⁵ and R²⁶ have the meaning according to claim 1 and LG denotes a leaving group, preferably a chlorine or bromine atom, in a reaction medium, optionally in the presence of at least one base, to yield at least one compound of the general formula Ih,

in which Y, T, U, V, W, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have the meaning according to claim 1 and n denotes 1, 2, 3 or 4 and said compound is optionally purified and/or isolated, and optionally at least one compound of the general formula Ih is reacted in a reaction medium with at least one compound of the general formula IX,

in which the phenyl residues are in each case substituted with 1 or 2 substituents mutually independently selected from the group consisting of methoxy, phenoxy, Cl, methyl and Br, preferably in each case with a phenoxy residue or methoxy residue, particularly preferably in each case with a methoxy residue in para position, or with phosphorus pentasulfide, to yield at least one compound of the general formula Ik,

in which Y, T, U, V, W, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have the meaning according to claim 1 and n denotes 1, 2, 3 or 4 and said compound is optionally purified and/or isolated.
 38. A process for the production of at least one compound according to claim 1, characterized in that at least one compound of the general formula X,

in which R⁵, U, T, V and W have the meaning according to claim 1, is reacted with at least one compound of the general formula VII,

in which Y, R¹, R², R³, R⁴, R²⁵ and R²⁶ have the meaning according to claim 1, in a reaction medium, optionally in the presence of at least one suitable coupling agent, optionally in the presence of at least one base, or with at least one compound of the general formula VIII,

in which Y, R¹, R², R³, R⁴, R²⁵ and R²⁶ have the meaning according to claim 1 and LG denotes a leaving group, preferably a chlorine or bromine atom, in a reaction medium, optionally in the presence of at least one base, to yield at least one compound of the general formula Im,

in which Y, T, U, V, W, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have the meaning according to claim 1 and said compound is optionally purified and/or isolated, and optionally at least one compound of the general formula Im is reacted in a reaction medium with at least one compound of the general formula IX,

in which the phenyl residues are in each case substituted with 1 or 2 substituents mutually independently selected from the group consisting of methoxy, phenoxy, Cl, methyl and Br, preferably in each case with a phenoxy residue or methoxy residue, particularly preferably in each case with a methoxy residue in para position, or with phosphorus pentasulfide, to yield at least one compound of the general formula In,

in which Y, T, U, V, W, R¹, R², R³, R⁴, R⁵, R²⁵ and R²⁶ have the meaning according to claim 1 and said compound is optionally purified and/or isolated.
 39. A pharmaceutical preparation containing at least one compound according to claim 1 and optionally one or more physiologically acceptable auxiliary substances.
 40. A pharmaceutical preparation according to claim 39 for the treatment and/or prevention of one or more diseases selected from the group consisting of pain, preferably of pain selected from the group consisting of acute pain, chronic pain, neuropathic pain and visceral pain; joint pain; hyperalgesia; allodynia; causalgia and migraine.
 41. A pharmaceutical preparation according to claim 39 for the treatment and/or prevention of one or more diseases selected from the group consisting of depression; neuropathy; nerve injury; neurodegenerative diseases, preferably selected from the group consisting of multiple sclerosis, Alzheimer's disease, Parkinson's disease and Huntington's chorea; cognitive dysfunction, preferably cognitive deficiency states, particularly preferably memory disorders; and epilepsy.
 42. A pharmaceutical preparation according to claim 39 for the treatment and/or prevention of one or more diseases selected from the group consisting of airways diseases, preferably selected from the group consisting of asthma, bronchitis and pulmonary inflammation; coughing; urinary incontinence; an overactive bladder (OAB); diseases and/or injuries of the gastrointestinal tract; duodenal ulcers; gastric ulcers; irritable bowel syndrome; strokes; eye irritation; skin irritation; neurotic skin conditions; allergic skin diseases; psoriasis; vitiligo; herpes simplex; inflammation, preferably inflammation of the intestines, the eyes, the bladder, the skin or the nasal mucosa; diarrhea; pruritus; osteoporosis; arthritis; osteoarthritis; rheumatic diseases; disorders of food intake, preferably selected from the group consisting of bulimia, cachexia, anorexia and obesity; dependency on medicines; abuse of medicines; withdrawal symptoms associated with dependency on medicines; development of tolerance towards medicines, preferably towards natural or synthetic opioids; dependency on drugs; drug abuse; withdrawal symptoms associated with dependency on drugs; dependency on alcohol; alcohol abuse and withdrawal symptoms associated with dependency on alcohol; for diuresis; for antinatriuresis; for influencing the cardiovascular system; for increasing vigilance; for the treatment of wounds and/or burns; for the treatment of severed nerves; for increasing libido; for modulating locomotor activity; for anxiolysis; for local anaesthesia and/or for inhibiting undesired side-effects, preferably selected from the group consisting of hyperthermia, high blood pressure and constriction of the bronchial tubes, triggered by the administration of agonists of the vanilloid receptor 1 (VR1/TRPV1 receptors), preferably selected from the group consisting of capsaicin, resiniferatoxin, olvanil, arvanil, SDZ-249665, SDZ-249482, nuvanil and capsavanil.
 43. Use of at least one compound according to one claim 1 for the production of a pharmaceutical preparation for the treatment and/or prevention of one or more diseases selected from the group consisting of pain, preferably of pain selected from the group consisting of acute pain, chronic pain, neuropathic pain and visceral pain; joint pain; hyperalgesia; allodynia; causalgia and migraine.
 44. Use of at least one compound according to claim 1 for the production of a pharmaceutical preparation for the treatment and/or prevention of one or more diseases selected from the group consisting of depression; neuropathy; nerve injury; neurodegenerative diseases, preferably selected from the group consisting of multiple sclerosis, Alzheimer's disease, Parkinson's disease and Huntington's chorea; cognitive dysfunction, preferably cognitive deficiency states, particularly preferably memory disorders; and epilepsy.
 45. Use of at least one compound according to claim 1 for the production of a pharmaceutical preparation for the treatment and/or prevention of one or more diseases selected from the group consisting of airways diseases, preferably selected from the group consisting of asthma, bronchitis and pulmonary inflammation; coughing; urinary incontinence; an overactive bladder (OAB); diseases and/or injuries of the gastrointestinal tract; duodenal ulcers; gastric ulcers; irritable bowel syndrome; strokes; eye irritation; skin irritation; neurotic skin conditions; allergic skin diseases; psoriasis; vitiligo; herpes simplex; inflammation, preferably inflammation of the intestines, the eyes, the bladder, the skin or the nasal mucosa; diarrhea; pruritus; osteoporosis; arthritis; osteoarthritis; rheumatic diseases; disorders of food intake, preferably selected from the group consisting of bulimia, cachexia, anorexia and obesity; dependency on medicines; abuse of medicines; withdrawal symptoms associated with dependency on medicines; development of tolerance towards medicines, preferably towards natural or synthetic opioids; dependency on drugs; drug abuse; withdrawal symptoms associated with dependency on drugs; dependency on alcohol; alcohol abuse and withdrawal symptoms associated with dependency on alcohol; for diuresis; for antinatriuresis; for influencing the cardiovascular system; for increasing vigilance; for the treatment of wounds and/or burns; for the treatment of severed nerves; for increasing libido; for modulating locomotor activity; for anxiolysis; for local anaesthesia and/or for inhibiting undesired side-effects, preferably selected from the group consisting of hyperthermia, high blood pressure and constriction of the bronchial tubes, triggered by the administration of agonists of the vanilloid receptor 1 (VR1/TRPV1 receptors), preferably selected from the group consisting of capsaicin, resiniferatoxin, olvanil, arvanil, SDZ-249665, SDZ-249482, nuvanil and capsavanil. 